Intermediate for making 3-oxo-4-aza-androst-1-ene...

C - Chemistry – Metallurgy – 07 – J

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C07J 73/00 (2006.01)

Patent

CA 2050822

Described is a new intermediate and new process for preparing 3-oxo-4-aza-androst-1-ene 17.beta.-ketones. The process involves converting the corresponding 17.beta.-alkyl carboxylate to the N-methoxy- N-methyl carboxamide and reacting this with an appro- priate Grignard reagent to form the desired ketone. The reaction can be conducted in "one pot", thus eliminating isolation of intermediates and avoiding the use of less stable intermediates, e.g., acid chlorides, acyl imidazolides and the like. The intermediate has the formula: Image II wherein R1 is hydrogen.

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