Disclosed is a process for preparing a compound of the formula:
wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula
wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence:
(a) a non-nucleophilic strong base;
(b) a chiral amino alcohol; and
(c) a compound having the formula
wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase. Also disclosed is a compound having the formula:
揭示了一种制备以下化合物的过程:
其中X1、X2、X3、X4和X5分别独立地选自H、卤素、烷基、烷氧基、芳基和芳氧基的组,R是保护基,在该过程中,具有以下公式的化合物:
其中X1、X2、X3、X4和X5如上定义,与以下物质以任意顺序处理:
(a) 非亲核强碱;
(b) 手性
氨基醇;和
(c) 具有以下公式的化合物:
其中L是离去基团,R如上定义。通过这种过程制备的化合物是制备法尼基蛋白转移酶
抑制剂的有用中间体。还揭示了具有以下公式的化合物: