Downstream synthetic route of 1122-10-7

As the paragraph descriping shows that 1122-10-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1122-10-7,3,4-Dibromo-1H-pyrrole-2,5-dione,as a common compound, the synthetic route is as follows.

1122-10-7, Somatostatin is peptide hormone which is known to exist ina form in which two cysteine residues within the molecule areattached via a disulfide bridge.1 mg of lyophilised somatostatin (Sigma-Aldrich) was resolubilised in 2 ml of 50mM NaHPO4, pH 6.2, 40% MeCN, 2.5% DMF. 500 jil were transferred to a Eppendorf reactiontube and diluted in the same buffer to a final concentration of0.25 mg/ml (152.6 jiM). 2.0 equivalents of TCEP (lOOx stock solution in 50 mM NaHPO4, pH 6.2, 40% MeCN) were added and the reaction incubated for 1 hour at ambient temperature. After reduction of the di sulfide bond 1.4 equivalentsof 2,3-dibromomaleimide (Sigma-Aldrich, lOOx stock solution in 50 mM NaHPO4, pH 6.2, 40% MeCN, 2.5% DMF)were added, the solution gently mixed and incubated for afurther 12 h at 4 C.Maleimide-bridged somatostatin was detected by EC-ESI65 MS (ES/ES). Controls included untreated peptide andsomatostatin treated with 2,3-dibromomaleimide or TCEPonly. Complete reduction was detected by the reaction of TCEP-treated peptide with maleimide (Sigma-Aldrich, lOOx stock solution in 50 mM NaRPO, pH 6.2, 40% MeCN, 2.5% DMF).Untreated somatostatin: [ES+]i638.04 (m/z 1), 819.82 (mlz 2), 546.95 (mlz 3). Maleimide-bridged somatostatin:[ES+] 1734.14 Da (mlz 1), 867.40 Da (mlz 2), 578.73 (mlz 3).

As the paragraph descriping shows that 1122-10-7 is playing an increasingly important role.

Reference£º
Patent; UCL Business Plc; Smith, Mark; Caddick, Stephen; Baker, James; Chudasama, Vijay; (80 pag.)US9295729; (2016); B2;,
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