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 (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 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; VAN BERKEL, Patricius Hendrikus Cornelis; HOWARD, Philip Wilson; (290 pag.)WO2016/166299; (2016); A1;,
Pyrroline – Wikipedia
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