| 摘要 |
1,230,630. 23 - Halo - 5# - cholanic acids. MERCK & CO. Inc. 21 Oct., 1968 [23 Oct., 1967 ; 2 Oct., 1968], No. 39947/70. Divided out of 1,230,628. Heading C2U. The invention comprises 23-halo-5#-cholanic acids and their non-toxic pharmacologically acceptable salts and C 1-5 alkyl esters, and their preparation from 5#-cholanic acid by treatment with a halogenating agent followed by treatment with water or with a C 1-5 alkanol according to whether a free acid or an ester is desired. The salts are prepared by reacting the acids with bases. The 23-bromo compounds are alternatively prepared by treating 5#-cholanic acid with thionyl chloride and bromine to give 23- bromo-5#-cholanoyl chloride and treating the latter with water or an alkanol to give a free acid or ester product. The 23-fluoro compounds are alternatively prepared from methyl 23- bromo-5#-cholanate by reaction with potassium fluoride and acidification to give a free acid product which may then be esterified. The esters of the invention may be saponified to give the free acids. |
