申请人:F. HOFFMANN-LA ROCHE & CO.
Aktiengesellschaft
公开号:EP0524495A1
公开(公告)日:1993-01-27
A process for the preparation of a tautomeric mixture of compounds of formulae
wherein W is hydrogen or C₆H₁₃,
which comprises treating a compound of the formula
wherein R is unsubstituted or substituted alkoxy, arylalkoxy, aryloxy or amine and R¹ is hydrogen or when R is alkoxy, substituted alkoxy, substituted amine, unsubstituted or substituted arylalkoxy R¹ can also be metal, with a compound of formula
wherein one of X and Y is a reducible group and the other is hydrogen or a reducible group, and Z is hydroxy or a leaving group,
and the obtained compound of formula
is treated with a low valent metal to form a tautomeric mixture of compounds of formulas I and Ia, which are useful in the synthesis of tetrahydrolipstatin.
一种制备式化合物同分异构体混合物的工艺
其中 W 为氢或 C₆H₁₃、
其中包括将式
其中 R 是未取代或取代的烷氧基、芳基烷氧基、芳氧基或胺,R¹是氢,或当 R 是烷氧基、取代的烷氧基、取代的胺、未取代或取代的芳基烷氧基时,R¹也可以是金属,用式化合物处理
其中 X 和 Y 的一个是还原基团,另一个是氢或还原基团,Z 是羟基或离去基团、
得到的式化合物
用低价金属处理,形成式 I 和 Ia 化合物的同分异构体混合物,可用于合成四氢司他丁。