PREGNANE DERIVATIVES AND PROCESS FOR THEIR PREPARATION.

摘要

Pregnane-2-carboxaldehyde derivatives (I) are new: where A1 is H and A2 is OH, acyloxy, lower alkoxycarbonyloxy, N-lower alkylcarbamoyloxy, N-arylcarbamoyloxy, N,N-di(lower alkyl) carbamoyloxy, tri-substd. silyloxy or alkoxymethoxy; or A1 is OH and A2 is H; or A1 and A2 together are =0; D1 is OH, acyloxy, lower alkylcarbonyloxy, N-lower alkylcarbamoyloxy, N-arylcarbamoyloxy, N,N-di(lower alkyl)carbamoyloxy, tri-substd. silyloxy or alkoxymethoxy, and D2 is H; or D1/D2 together may forma double bond or epoxy; D3 is H and D4 is OH; or D3/D4 together are a double bond or epoxy; D5 is H and D6 is OH, lower alkoxycarbonyloxy, acyloxy, N-lower alkylcarbamoyloxy, N-acrylcarbamoyloxy, N,N-di(lower alkyl)-carbamoyloxy; or D5/D6 together are a souble bond or epoxy; D4/D5 together may be a double bond; D7 is H or D6/D7 together may be a double bond; X1 and X2 are each lower alkoxy or together form =0 or alkylenedioxy. The following are preferred: (a) A1/A2=0, D1/D2 and D3/D4 are double bonds, D5=H, D6=OH, D7=H; (b) A1/A2=0, D1/D2 is a double bond or epoxy, D3/D4 and D5/D6 are double bonds, D7=H; (c) A1=H and A2=OH or lower alkanoyloxy, or A1/A2=0, D1/D2 is epoxy, D3/D4 is a double bond, D5/D6 is epoxy, D7=H; (d) A1=OH, A2=H, D1/D2 is epoxy, D3/D4 and D5/D6 are double bonds, D7=H; (e) D1/D2 and D3/D4 are epoxy, D5/D6 is a double bond, D7=H; (f) D2=H, D3=H, D4=OH, D5/D6 is a double bond, D7=H, A1=H; (g) D2=D3=H, D4/D5 is a double bond, D7=H, A1=H; (h) D1/D2 is epoxy, A1 is H, A2 is H or lower alkanoyloxy, D3=H, D4/D5 is a double bond, D7=H, or D6/D7 are a double bond; (i) D2=H, A1=H, D3=H, D4/D5 and D6/D7 are double bonds.