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US 4,225,524 AGranted
Steroid derivatives and process for preparing the same
AssigneeChugai Seiyaku Kabushiki Kaisha
InventorsKiyoshige Ochi, Isao Matsunaga, Minoru Shindo, Chikara Kaneko
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Abstract
Steroid derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are as defined hereunder which is useful for easily producing a wide variety of active vitamin D, and a process for preparing the same are disclosed.
Claims19
A process for preparing a steroid derivative represented by the formula ##STR9## wherein R.sup.1 is hydrogen or a protecting group for hydroxyl radical and R.sup.2 is ##STR10## in which R.sup.3 is hydrogen or a protecting group for hydroxyl radical, which comproses a method selected from the class consisting of:
- (1) reacting a compound represented by the formula ##STR11## wherein R.sup.4 is a protecting group for hydroxy radical, with an acid selected from the group consisting of phosphorus oxychloride, thionyl chloride, methane sulfonic acid, p-toluenesulfonic acid, methane sulfonylchloride, p-toluenesulfonyl chloride, phosphoric anhydride and sulfuric acid;
- and, optionally, hydrolyzing the product;
- (2) reacting a compound represented by the formula ##STR12## wherein R.sup.4 is as defined above, with methanesulfonyl chloride or p-toluenesulfonyl chloride, heating the product to subject it to eliminating reaction and, optionally, hydrolyzing the product;
- or
- (3) reacting a compound represented by the formula ##STR13## wherein R.sup.4 is as defined above, with an acid selected from the group consisting of phosphorus oxychloride, thionyl chloride, methane sulfonic acid, p-toluenesulfonic acid, methane sulfonylchloride, p-toluenesulfonyl chloride, phosphoric anhydride and sulfuric acid;
- reacting the resulting compound represented by the formula ##STR14## wherein R.sup.4 is as defined above with a mercuric salt, reducing the resulting compound with an alkali metal borohydride and, optionally, hydrolyzing the product.
3 more elements
Dependencies are inferred from the claim text.