| 摘要 |
1498239 D-homo steroid amine salts F HOFFMANN-LA ROCHE & CO AG 28 Oct 1975 [29 Oct 1974] 44288/75 Heading C2U The invention comprises the mono and bis quaternary salts of diamines of Formula I and also the acid addition salts of the monoquaternary salts (R<SP>1</SP>, R<SP>2</SP>, R<SP>4</SP> and R<SP>5</SP> are each H, C 1-10 alkyl or C 7-10 aralkyl, or NR<SP>1</SP>R<SP>2</SP> or NR<SP>4</SP>R<SP>5</SP> is a heterocyclic group; R<SP>3</SP> is H or acyl; R<SP>6</SP> is oxo (H, α-OR<SP>7</SP>) or (H, #-OR<SP>7</SP>) where R<SP>7</SP> is H or acyl); and their preparation by salification of the diamines (e.g. with an alkyl halide) and if desired reducing a 17a-oxo group or acylating a 3- or 17ahydroxy group. 3# - Hydroxy - D - homo - 5α - androstan- 17a - one#3# - hydroxy - 17a,17a - ethylenedioxy- D - homo - 5α - androstane#3# - tosyloxy- 17a,17a - ethylenedioxy - D - homo - 5α - androstane#17a,17a - ethylenedixoy - D - homo - 5α- androst - 2 - ene#D - homo - 5α - androst - 2- en - 17a - one#17a - acetoxy - D - homo - 5α androsta - 2,17(17a) - diene#17α# - acetoxy- 2α,3α; 17a,17aα - diepoxy - D - homo - 5α- androstane#(i) 3α - hydroxy - 2#,17# - bis- (dimethylamino) - D - homo - 5α - androstan - 17aone or (ii) 3α - hydroxy - 2#.17# - dipiperidino- D - homo - 5α - androstan - 17a - one; then (ii)# 3α,17α# - dihydroxy - 2#,17# - dipiperidino - D- homo - 5α - androstane#3α,17a# - diacetoxy- 2#,17#-dipiperidino-D-homo-5α-androstane. 3#,17α# - Dihydroxy - D - homo - 5α - androstane - 3#,17α# - ditosyloxy - D - homo - 5α- androstane#D - homo - 5α - androsta - 2,17(17a)- diene#(i) 2α,3α; 17α,17aα - diepoxy - D- homo - 5α - androstane and (ii) its 17#,17a#- isomer; then (i) #3α,17aα - dihydroxy- 2#,17# - dipiperidino - D - homo - 5α - androstane#3α,17aα - diacetoxy - 2#,17# - dipiperidino-D-homo-5α-androstane. Anaesthetic parenteral compositions comprise a carrier and a compound of the invention. |
