新产品编号:1300913
Chemical Name: (3R,6S,8aS)-6-(Benzylsulfonamido)-N-(3-guanidinopropyl)-5-oxohexahydro-5H-thiazolo[3,2-a]pyridine-3-carboxamide bis(trifluoroacetate)
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Originator)
合成路线:Coupling of thiazolopyridine (I) with amine (II) in the presence of EDC and HOBt provided amide (III).Deprotection of the Fmoc group of (III) was effected with piperidine in CH2Cl2 and the resulting amine (IV) was condensed with benzylsulfonyl chloride (V) to afford sulfonamide (VI).Finally,both Boc protecting groups of (VI) were removed with TFA to yield the title guanidine as the bis(trifluoroacetate) salt.
📌 参考资料/链接:
参考文献标题:Rational design,synthesis,and X-ray structure of selective noncovalent thrombin inhibitors
文献作者:Wagner,J.; Kallen,J.; Ehrhardt,C.; Evenou,J.-P.; Wagner,D.
参考来源:J Med Chem 1998,41(19),3664