新产品编号:403919

Chemical Name: 2(R)-[4-(5-Chloro-2-pyridinyl)-1-piperazinylsulfonamido]-N-hydroxy-3-methylbutyramide
CAS No. 210913-38-5
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator), Roche (Originator)
合成路线:Treatment of D-valine methyl ester (I) with chlorosulfonic acid and then with phosphorus pentachloride produced valinesulfamoyl cloride (II).This was condensed with N-(5-chloro-2-pyridinyl)piperazine (III) to afford sulfamide (IV).Basic hydrolysis of the methyl ester of (IV) gave carboxylic acid (V),which was further converted to acid chloride (VI) using oxalyl chloride in the presence of DMF.Finally,the title hydroxamic acid was obtained by condensation with N,O-bis(trimethylsilyl)hydroxylamine,followed by desilylation with MeOH.
📌 参考资料/链接:
参考文献标题:Sulfamide-metalloprotease inhibitors
文献作者:Castelhano,A.L.; Hendricks,R.T.; Melnick,M.J.; Campbell,J.A.; Walker,K.A.M.; Broka,C.A.; Chen,J.J.(Agouron Pharmaceuticals,Inc.; F.Hoffmann-La Roche AG)
参考来源:DE 19802350; EP 0958287; US 5998412; WO 9832748