PURPOSE: To obtain a new nitromethylene compd. as a synthesis intermediate of an acetoxy-oxocorticosteroid compd. useful as pharmaceuticals.
CONSTITUTION: The nitromethylene compd. is a compd. of formula I (where R1 is H, a 1-4 C alkyl, etc.; R2 is a 1-4 C alkyl; and X is C or C-C), e.g. 3β- hydroxy-17-(nitromethylene)androsta-5-ene. The compd. is obtd. by allowing a ketone nitromethylating agent made of nitromethane to react with a compd. of formula II in the presence of a basic bifunctional catalyst, preferably ethylenediamine. When an aldehyde of the formula RCHO (where R is H or 1-18 C alkyl), an esterifying agent, a nitro group reducing agent and an oxime functional group cleaving agent are successively allowed to react with the compd. of the formula I starting material, a 21-acetoxy-20-oxocorticosteroid deriv. of formula III (where AC is the residue of a 1-18 C acyl) useful as pharmaceuticals is obtd.
UIRIAMU BURANKUSU MAZAUERU
SAMIIRU ZAARU ZAARU
