摘要 |
1,192,062. #<SP>1,4</SP> - 3 - Hydroxysteroids. AMERICAN HOME PRODUCTS CORP. 24 April, 1967 [13 March, 1967], No. 63268/69. Divided out of 1,192,061. Heading C2U. The invention comprises compounds of formula wherein R is C 1-5 alkyl; R<SP>1</SP>, R<SP>2</SP> and R<SP>3</SP> are H or C 1-5 alkyl; and X is a radical selected from wherein R<SP>4</SP> is H or C 1-5 alkyl; A is protected carbonyl or C(α-R<SP>6</SP>)(#-OH) where R<SP>6</SP> is a C 1-5 alkyl, alkenyl, alkynyl or chloroalkynyl group; B is CH 2 , CHOH or protected carbonyl; provided that when B is CH 2 , A is C(α-R<SP>6</SP>)(#-OH) where R<SP>6</SP> is C 2-5 alkyl, and that when B is CHOH, A is protected carbonyl or C(α-R<SP>6</SP>)- (#-OH) where R<SP>6</SP> is C 2-5 alkyl; and wherein R<SP>4</SP> and B are as above; D is CH 2 , CHOH or CHF; R<SP>7</SP> is H(OH) or protected carbonyl; R<SP>8</SP> and R<SP>9</SP> are each H, OH or protected OH; R<SP>10</SP> is H or C 1-5 alkyl; and R<SP>11</SP> is H or F; provided that when B is CHOH, D is CH 2 and R<SP>7</SP> is H(OH) then R<SP>8</SP> and R<SP>9</SP> are each H or protected OH, and that when B is CHOH, D is CH 2 and R<SP>7</SP> is protected carbonyl then R<SP>8</SP> and R<SP>9</SP> are both H. These compounds are prepared by reduction of the corresponding 1,4-dien-3-ones using aluminium hydride or a complex aluminium hydride at a temp. below 10‹ C. The products may be acylated. |