A novel and practical route to A-ring enyne synthon for 1α,25-dihydroxyvitamin D3 analogs: Synthesis of A-ring diastereomers of 1α,25-dihydroxyvitamin D3 and 2-methyl-1,25-dihydroxyvitamin D3

作者: Katsuhiro Konno , Shojiro Maki , Toshie Fujishima , Zhaopeng Liu , Daishiro Miura

DOI: 10.1016/S0960-894X(97)10204-9

关键词:

摘要: A novel and practical route to the A-ring enyne synthon (2), which can be versatile for a variety of analogs 1α,25-dihydroxyvitamin D3 (1), was developed. This method led an improved synthesis diastereomers 1, compounds 13–15, new analogs, 2-methyl-1,25-dihydroxyvitamin (4) with its all possible diastereomers. The biological evaluation 2-methyl showed ααβ-isomer more potent than 1.

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