Synthesis of 21-nor-22-oxa-1α,25-dihydroxyvitamin D<sub>3</sub> derivatives in quest of a drug with low calcemic activity期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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Synthesis of 21-nor-22-oxa-1α,25-dihydroxyvitamin D₃ derivatives in quest of a drug with low calcemic activity

Authors:	Hitoshi Shimizu Kazuki Shimizu Atsuko Sugita Tsuyoshi Yamauchi Kazumi Morikawa

Institution:	^a Synthetic Technology Research Department, Chugai Pharmaceutical Co., Ltd, 5-5-1 Ukima, Kita-Ku, Tokyo 115-8543, Japan ^b Chemistry Research Department I and Pharmaceutical Research Department II, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan

Abstract:	Two 21-nor-22-oxa-1α,25-dihydroxyvitamin D₃ derivatives have been synthesized in quest of a drug with lower calcemic activity than Maxacalcitol, 22-oxa-1α,25-dihydroxyvitamin D₃, being used as antihyperparathyroidism and antipsoriatic drug. Of two 21-nor products obtained, the product carrying one carbon elongated side chain with diethylcarbinol moiety has been found to exhibit comparable differentiation-inducing activity to Maxacalcitol with much lower exhibition of calcemic activity.

Keywords:	Vitamin D₃ derivative 22-Oxavitamin D₃ derivatives Separation of activity Calcemic activity Differentiation-inducing activity
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