首页> 外国专利> Process for the preparation of 1alpha, 25-dihydroxycholecalciferol, a compound with improved antirachitic properties compared to vitamin D2, and D3, and which has value as a ADDING substance for impregnation agents, and relates to intermediates for their preparation

Process for the preparation of 1alpha, 25-dihydroxycholecalciferol, a compound with improved antirachitic properties compared to vitamin D2, and D3, and which has value as a ADDING substance for impregnation agents, and relates to intermediates for their preparation

机译:1alpha,25-dihydroxycholecalciferol的制备方法,该化合物具有比维生素D2和D3更高的抗花生四烯酸性质,并且具有作为浸渍剂添加物质的价值,并且涉及其制备中间体

摘要

1496319 Cholesta-5,7-diene derivative WISCONSIN ALUMNI RESEARCH FOUNDATION 27 Feb 1976 [28 Feb 1975] 06294/77 Divided out of 1496317 Heading C2U The invention comprises cholesta-5,7-diene- 1,3#,25 - triol (I) and its preparation from cholesta - 1,5,7 - triene - 3#,25 - diol (VII) by reaction with a 4-substituted-1,2,4-triazoline- 3,5-dione to give V infra, epoxidation of which gives IV infra, reduction of which with a metal hydride (e.g. LiAlH 4 or LiBH 4 ) yields I (R is alkyl, aryl or monosubstituted aryl). IV may be accompanied by 1#,2#-epoxy epimer which is separated chromatographically. Conversion of I to 1,25-dihydroxycholecalciferol is as described in parent Specification. Compound VII and precursors thereof are the subject of Specification 1,496,318.
机译:1496319 Cholesta-5,7-二烯衍生物WISCONSIN校友研究基金会1976年2月27日[1975年2月28日] 06294/77除以1496317标题C2U,本发明包括cholesta-5,7-diene-1,3#,25-triol( I)及其通过与4-取代的1,2,4,3-三唑啉-3,5-二酮反应由胆甾型-1,5,7-三烯-3#,25-二醇(VII)制备而得到V infra ,其环氧化得到下面的IV,用金属氢化物(例如LiAlH 4或LiBH 4)还原得到IV(R是烷基,芳基或单取代的芳基)。 IV可能伴有色谱分离的1#,2#环氧差向异构体。 I到1,25-二羟基胆钙化固醇的转化如母说明书中所述。化合物VII及其前体是说明书1,496,318的主题。

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