Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

EDCI hydrochloride (39 mg, 0.197 mmol, leq.) was added to a suspension of maleimide-PEG8-acid (117 mg, 0.197 mmol, leq.) in dry CH2CI2 (5 mL) under argon atmosphere. The mixture was stirredfor 30 mm at room temperature before PBD 13 (250 mg, 0.197 mmol) was added. Stirring was maintained until the reaction was complete (usually 5 hours). The reaction was diluted with CH2CI2 and the organic phase was washed with H20 and brine before being dried over Mg504, filtered and excess solvent removed by rotary evaporation under reduced pressure. The product was purified by careful silica gel chromatography (gradient elution: 100% CHCI3 to 9:1 v/v CHCI3/MeOH)to affordpure product 14(273.8mg, 75% yield). Analytical data: ES = 1.99 mi m/z 1863.95 [M+Na].

1334177-86-4, As the paragraph descriping shows that 1334177-86-4 is playing an increasingly important role.

Reference£º
Patent; MEDIMMUNE LIMITED; HOWARD, Philip Wilson; CAILLEAU, Thais; (159 pag.)WO2017/129652; (2017); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7544-75-4,3,4-Dihydro-2H-pyrrol-5-amine hydrochloride,as a common compound, the synthetic route is as follows.

Prepare 2-iminopyrrolidine hydrochloride (6. 98 g, 57.8 mmol) according to Callahan, et al., J. Med. Chem. 2002,45, 999-1001) and combine 2-bromoacetophenone (3.8 g, 19.3 mmol) with Na2CO3 (8.2 g, 77.2 mmol) in dry DMF (25 [ML)] and heat at [80C] for 18 hours. Then, cool the mixture to room temperature, add water (60 mL), and extract with EtOAc (3 x 100 mL). Concentrate the combined organic layers in vacuo, dilute the residue with ether (100 mL), and wash with cooled water (3 x 80 mL). Concentrate the organic layer in vacuo to give a white solid, 3.2 g, 89 [%] yield. MS [(ES+)] : [IIZLZ] = 185. 1 [(M+H) +], 7544-75-4

7544-75-4 3,4-Dihydro-2H-pyrrol-5-amine hydrochloride 12778905, apyrrolines compound, is more and more widely used in various.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2004/14900; (2004); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.17057-04-4,4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid,as a common compound, the synthetic route is as follows.

General procedure: Equimolar quantities of maleimide (2) and nitrones (5a-k and 6a-k) were refluxed in toluene (20 ml) and ethyl alcohol (5 ml) for 8-10 h (TLC monitoring using petroleum ether and hexane 1:1) followed by cooling with addition of dry ether. The products (7a-k and 8a-k) were separated out after filtration and recrystallized from toluene and petroleum ether mixture (1:1) to yield cis-isomers (7aa-7ka and 8aa-8ka). The mother liquor on further work up provided trans-isomers which were recrystallized from ethanol and diethyl ether mixture (1:1) (7aa’-7ka’ and 8aa’-8ka’) (Fig. 3).7 These stereoisomers were characterized by their 1H NMR, IR and mass spectra in addition to their melting points and elementary analysis. These stereoisomers have identical IR spectra and elemental analysis but differ in their melting points, 1H NMR and mass spectra.

17057-04-4, 17057-04-4 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid 86925, apyrrolines compound, is more and more widely used in various.

Reference£º
Article; Anand, Preet; Singh, Baldev; Bioorganic and Medicinal Chemistry; vol. 20; 1; (2012); p. 521 – 530;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

57079-01-3, 11-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)undecanoic acid is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57079-01-3, N-Maleimidyunndecanoic acid (171.4 g, 0.61 mol) and ethyl acetate (300 ml) were added to a 500 ml three-necked flaskand then thionyl chloride (142 g, 1.21 mol) A lot of gas released.After refluxing for 3h,almost no gas was released, the ethyl acetate was removed by concentration and excess thionyl chloride was added, and 200 ml of ethyl acetate was added to remove the residualacidonce toobtain crude N-maleimido undecanoyl chloride.The crude product was dissolved in 200 ml of ethyl acetate and added dropwise to a solution of N-hydroxysuccinimide (92 g, 0.8 mol) and diisopropylethylamine (129 g, 1.0 mol) in 300 ml of ethyl acetate. IceWater cooling control temperature does not exceed 20 , drip finished room temperature stirring 3h.The reaction mixture was washed with 200 ml of water to remove diisopropylethylamine hydrochloride, 100 ml of 1N hydrochloric acid to remove excess diisopropylethylamine, 200 ml of saturated saline, washed, dried and concentrated to give196 g of a white solid, ethyl acetate and petroleum Ether mixed solvent was recrystallized to give a white solid 152g,HPLC purity 98.2%, yield 66.1%.

As the paragraph descriping shows that 57079-01-3 is playing an increasingly important role.

Reference£º
Patent; Suzhou Haofan Biological Technology Co., Ltd.; Lv Minjie; Zhang Haiyan; Wang Guichun; Sun Fangchao; (10 pag.)CN105037237; (2017); B;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

1334177-86-4, 1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Chloroform (4.1 ml) and methanol (0.2 ml) were added to 23, followed by mal-amidopeg8-acid (238 mg, 0.394 mmol, 2.2 eq) and EDCI (85.0 mg, 0.443 mmol, 2.48 eq). The reaction was allowed to proceed at room temperature for 45 min when completion was observed by LCMS. The reaction mixture was concentrated (2 ml), loaded on a 3g biotage 20 silica samplet and dried under vacuum. The samplet was loaded on a 25g Ultra Biotage column, and eluted (gradient 10/90 to 58/42 of 20% MeOH in DCM I DCM in 12CV; Elution at around 55% of 20% MeOH). All fractions were analysed by TLC (10% MeOH in DCM). The pure fractions were pooled. The solvent was removed by evaporation to give 24 (250 mg, 0.105 mmol, 58.8% Yield). Analytical Data: LC/MS, 15 min method, RT 6.20 min; MS 25 (ES+) m/z (relative intensity) 1191.5 ([M + 2Hf+¡¤, 1 00); 1H NMR (400 MHz, DMSO-d6) o 9.92 (s, 2H), 8.16 (d, J = 6.9 Hz, 2H), 7.99 (t, J = 5.5 Hz, 2H), 7.86 (d, J = 8.6 Hz, 2H), 7.68 – 7.42 (m, 4H), 7.39- 7.11 (m, 4H), 7.07 (s, 2H), 7.00 (s, 4H), 6.81 (s, 2H), 6.60 (s, 2H), 5.46- 5.30 (m, 2H), 5.21 -4.79 (m, 8H), 4.39 (t, J = 7.0 Hz, 2H), 4.22 (dd, J = 8.7, 6.7 Hz, 2H), 4.15- 3.88 (m, 8H), 3.77 (s, 6H), 3.65- 3.55 (m, 8H), 3.54- 3.40 (m, 58H), 3.37 (t, J 30 = 5.9 Hz, 4H), 3.15 (q, J = 5.8 Hz, 4H), 2.95-2.79 (m, 2H), 2.57-2.52 (m, 2H), 2.492.37 (m, 4H), 2.37-2.29 (m, 4H), 2.22-2.10 (m, 2H), 2.03- 1.88 (m, 2H), 1.30 (d, J = 7.0 Hz, 6H), 0.85 (dd, J = 15.3, 6.7 Hz, 12H)., 1334177-86-4

As the paragraph descriping shows that 1334177-86-4 is playing an increasingly important role.

Reference£º
Patent; MEDIMMUNE LIMITED; DIMASI, Nazzareno; HOWARD, Philip Wilson; MASTERSON, Luke; TIBERGHIEN, Arnaud Charles; VIJAYAKRISHNAN, Balakumar; WHITE, Jason; (135 pag.)WO2019/34764; (2019); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

(e) 1-(3-(2, 5-dioxo-2 , 5-dihydro- 1H-pyrrol- 1-yI)propanamido)-N-((2S)- 1-(((2S) – 1-((4-(7- methoxy-8-(3-((7-methoxy-2-(4-(4-methylpiperazin- 1-yI)phenyl)-5-oxo-5, 1 la-dihydro- 1H- benzo[e]pyrrolo[1, 2-a][1, 4]diazepin-8-yI) oxy)propoxy) -5-oxo-5, 1 la-dihydro- 1H- benzo[e]pyrrolo[1, 2-a][1, 4]diazepin-2-yI)phenyl)amino) – 1-oxopropan-2-yI)amino)-3-methyl- 1- oxobutan-2-yI)-3, 6,9, 12,15, 18,21, 24-octaoxaheptacosan-2 7-amide (86)EDCI hydrochloride (8 mg, 0.042 mmol) was added to a suspension of Maleimide-PEG8-acid (25 mg, 0.042 mmol) in dry CH2CI2 (4 mL) under argon atmosphere. PBD 85 (42 mg, crude) was added straight away and stirring was maintained until the reaction was complete (3 hours). The reaction was diluted with CH2CI2 and the organic phase was washed with H20 and brine before being dried over MgSO4, filtered and excess solvent removed by rotary evaporation under reduced pressure by rotary evaporation under reduced pressure. The product was purified by careful silica gel chromatography (slow elution starting with 100% CHCI3 up to 9:1 CHCI3/MeOH) followed by reverse phase HPLC to remove unreacted maleimide-PEG8-acid. The product 86 was isolated in 10% over two steps (6.6 mg). LC/MS 1.16 mm (ES+) m/z (relative intensity) 770.20 ([M+ 2H], 40%)., 1334177-86-4

1334177-86-4 1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid 51340955, apyrrolines compound, is more and more widely used in various.

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; VAN BERKEL, Patricius Henrikus Cornelis; HOWARD, Philip Wilson; WILLIAMS, David G; WO2015/159076; (2015); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

17057-04-4, 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Equimolar quantities of maleimide (2) and nitrones (5a-k and 6a-k) were refluxed in toluene (20 ml) and ethyl alcohol (5 ml) for 8-10 h (TLC monitoring using petroleum ether and hexane 1:1) followed by cooling with addition of dry ether. The products (7a-k and 8a-k) were separated out after filtration and recrystallized from toluene and petroleum ether mixture (1:1) to yield cis-isomers (7aa-7ka and 8aa-8ka). The mother liquor on further work up provided trans-isomers which were recrystallized from ethanol and diethyl ether mixture (1:1) (7aa’-7ka’ and 8aa’-8ka’) (Fig. 3).7 These stereoisomers were characterized by their 1H NMR, IR and mass spectra in addition to their melting points and elementary analysis. These stereoisomers have identical IR spectra and elemental analysis but differ in their melting points, 1H NMR and mass spectra., 17057-04-4

17057-04-4 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid 86925, apyrrolines compound, is more and more widely used in various.

Reference£º
Article; Anand, Preet; Singh, Baldev; Bioorganic and Medicinal Chemistry; vol. 20; 1; (2012); p. 521 – 530;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

DCM (10.00 ml) and methanol (0.4 ml) were added to 36 (393 mg, 0.305 mmol), followed by mal-amido-peg8-acid (380 mg, 0.628 mmol, 2.06 eq) and EDCI (128 mg, 0.668 mmol, 2.2 eq). The reaction was allowed to proceed at room temperature for 4h when completion 15 was observed by LCMS. Ammonium chloride in water (30 ml, 6 mass%) was added and the mixture was stirred vigorously. The mixture was decanted in a biotage phase separation cartridge. The DCM layer was evaporated to dryness under vacuum and the crude residue was purified by chromatography (25g Ultra gradient 15/85 to 100/0 of 20% MeOH in DCM I DCM in 12CV; hold at elution around 48%). The fractions were analysed 20 by TLC (1 0% MeOH in DCM). The pure fractions were pooled. The solvent was removed by evaporation. The residue was purified further by reverse phase preparative HPLC (gradient 15 to 75% water/acetonitrile + 0.01% formic acid) followed by freeze-drying and aliquoted from DCM to give 37 (516 mg, 0.212 mmol, 69.4% Yield) as a white foam. The purity was 97.65%. Analytical Data: LC/MS, 15 min method, RT 6.61 min; MS (ES+) m/z 25 (relative intensity) 1219.7 ([M + 2Hf+¡¤, 100); 1H NMR (400 MHz, DMSO-d6) o 9.92 (s, 2H), 8.17 (d, J = 6.9 Hz, 2H), 8.01 (t, J = 5.6 Hz, 2H), 7.87 (d, J = 8.7 Hz, 2H), 7.72- 7.44 (m, 4H), 7.39- 7.10 (m, 4H), 7.05 (s, 2H), 7.00 (s, 4H), 6.76 (s, 2H), 6.66- 6.46 (m, 2H), 5.56 (d, J = 7.1 Hz, 2H), 5.34 (dd, J = 9.7, 5.9 Hz, 2H), 5.21 – 4.70 (m, 4H), 4.39 (t, J = 7.0 Hz, 2H), 4.22 (dd, J = 8.7, 6.7 Hz, 2H), 4.15-4.01 (m, 2H), 3.94 (d, J = 15.3 Hz, 4H), 3.8630 3.72 (m, 8H), 3.60 (t, J = 7.3 Hz, 8H), 3.55- 3.42 (m, 58H), 3.37 (t, J = 5.9 Hz, 4H), 3.15 (q, J = 5.8 Hz, 4H), 2.76-2.56 (m, 4H), 2.46 (t, J = 6.8 Hz, 2H), 2.40 (t, J = 6.5 Hz, 2H), 2.36- 2.29 (m, 4H), 1.96 (q, J = 6.7 Hz, 2H), 1.78 (s, 4H), 1.66 (d, J = 6.6 Hz, 6H), 1.57 (d, J = 8.6 Hz, 2H), 1.30 (d, J = 7.0 Hz, 6H), 0.85 (dd, J = 15.2, 6.7 Hz, 12H)., 1334177-86-4

The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MEDIMMUNE LIMITED; DIMASI, Nazzareno; HOWARD, Philip Wilson; MASTERSON, Luke; TIBERGHIEN, Arnaud Charles; VIJAYAKRISHNAN, Balakumar; WHITE, Jason; (135 pag.)WO2019/34764; (2019); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

134272-64-3, N-(2-Aminoethyl)maleimide Hydrochloride is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

GA16OH was used for the synthesis of GA16-MA to increase the solubility in hydrocarbon. To asolution of GA16OH (0.5g, 0.60mmol) in dichloromethane (10 mL) was added N,Ndiisopropylethylamine(0.85ml, 6mmol). The mixture was treated with N-(3-dimethylaminopropyl)-N?-ethylcarbodiimide hydrochloride (0.19g, 1mmol), 1-hydroxybenzotriazole (0.13g, 1mmol) and N-(2-aminoethyl)maleimide hydrochloride (0.116g,0.66mmol) and stirred at room temperature overnight. The reaction was quenched with droplet ofHCl (1M) solution and washed with water for three times. The organic portion was dried overNa2SO4. The crude material was purified by silica gel column chromatography using hexane andEtOAc (4/1 to 3/1).1H NMR (400MHz, CDCl3): delta 6.96 (s, 2H), 6.73 (s, 2H), 6.58 (t, J=4.6 Hz, 1H), 4.04-3.96 (m,6H), 3.84-3.82 (m, 2H), 3.66-3.62 (m, 2H), 1.83-1.71 (m, 6H), 1.49-1.45 (m, 6H), 1.37-1.26 (m,72H), 0.90-0.86 (m, 9H)HRMS (ESI): Calculated for C61H108N2O6 ([M+H]+): 965.8286 , found 965.8264.

134272-64-3, The synthetic route of 134272-64-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Zhang, Qifan; Scigliano, Anita; Biver, Tarita; Pucci, Andrea; Swager, Timothy M.; Bioorganic and Medicinal Chemistry; (2018); p. 5307 – 5313;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

N-(3-Dimethylaminopropyl)-N?-ethylcarbodiimide (28 mg, 0.146 mmol, I eq) was added to asolution of 42 (203 mg, 0.146 mmol) and maleimide-PEG8 acid (87 mg, 0.146 mmol) inchloroform (5 mL). The reaction was stirred for 1.5 h then diluted with chloroform (50 mL), washed with water (50 mL), brine (30 mL), dried over magnesium sulphate, filtered and evaporated. Flash chromatography [gradient elution 100% DCM to 90% DCM/I0% methanol] gave 43 as a pale yellow solid (205 mg, 72%). LC/MS: RT 5.75 mm; MS (ES+)m/z (relative intensity) 982.90 (100), 1963.70 (5)., 1334177-86-4

The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SPIROGEN SARL; ADC THERAPEUTICS SARL; HOWARD, Philip Wilson; VAN BERKEL, Patricius Hendrikus Cornelis; WO2015/52532; (2015); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem