| 摘要 |
PURPOSE: To obtain a vitamin D3 derivative expressed by a specific formula, having bone-salt increasing effect, thus useful as a therapeutic agent for osteoporosis. CONSTITUTION: This compound is expressed by formula I [R1 and R2 are each a 1-4C alkyl; R3 is OH, a halogen, cyano, 1-4C alkoxyl, amino or (acylamino- substituted) 1-7C alkoxyl], e.g. 26,27-dimethyl-2β-(3-hydroxypropoxy)-1α,3β,25 trihydroxy-9,10-seco-cholesta-5,7,10(19)-toluene. It is preferable that this compound of formula I is obtained, for example, by the following process: a substituent is introduced onto the 2-site of an epoxy compound of formula II followed by protecting the OH group of the resultant compound and subjecting the resultant OH-protected compound to Grignard type reaction to form a compound of formula III, which is then deprotected at need, followed by conducting an irradiation with light and thermal isomerization.
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