Vincze I, Hackler L, Szendi Z, Schneider G
Department of Organic Chemistry, Attila József University, Szeged, Hungary.
Steroids. 1996 Dec;61(12):697-702. doi: 10.1016/s0039-128x(96)00202-4.
Aminosteroids were prepared and acylated with protected amino acids by means of the mixed anhydride or the active ester method. The tert-butyloxycarbonyl- (BOC) protecting group was eliminated by acidolysis, and the benzyloxycarbonyl- (Z) group by catalytic hydrogenation. 3 beta- and 6 beta-Glycylamidosteroids were prepared by indirect amination of chloroacetamido derivatives, formed by the Ritter reaction on the corresponding 3 alpha,5 alpha-cyclo and 5 alpha,6 alpha-epoxy steroids. Water-soluble double salts were produced from the compounds for pharmacological investigations.
制备了氨基甾体，并通过混合酸酐法或活性酯法用保护氨基酸进行酰化。叔丁氧羰基（BOC）保护基通过酸解除去，苄氧羰基（Z）保护基通过催化氢化除去。3β-和6β-甘氨酰胺甾体是通过对相应的3α,5α-环和5α,6α-环氧甾体进行 Ritter 反应形成的氯乙酰胺衍生物间接胺化制备的。为了进行药理研究，从这些化合物中制备了水溶性复盐。
