Synthesis of 6-methylene derivatives of...

C - Chemistry – Metallurgy – 07 – J

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C07J 1/00 (2006.01) C07J 75/00 (2006.01)

Patent

CA 1319680

A B S T R A C T The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) Image (I) wherein each of R1 and R3, independently, is hydrogen or C1-C6 alkyl; R2 is hydrogen, halogen or C1-C6 alkyl; and R4 is hydrogen or fluorine; the process comprising submitting to Mannich reaction a com- pound of formula (II) Image (II) wherein R1, R2, R3 and R4 are as defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA.4 -steroid derivative thus obtained, by methods known per se.

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