Physiologically active substance TAN-931, its derivatives, their

Details Physiologically active substance TAN-931, its derivatives, their Physiologically active substance TAN-931, its derivatives, their

1991-02-27

1993-03-23

Killos, Paul J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

435183, 560 35, 560 54, C07C 6976

Patent

active

051965640

ABSTRACT:
A novel compound of the formula (I): ##STR1## wherein R.sub.1 is esterified carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.

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Journal of the Chemical Society, Section C. Organic Chemistry, Part II, pp. 1175-1182.
Chemical Abstracts, vol. 87, No. 11, Sep. 12, 1977, p. 564, Abstract No. 84687m, Columbus, Ohio, U.S.; & JP-A-77 31 059 (Mitsubishi Gas Chemical Co., Inc.) Sep. 3, 1977.
Kanamaru et al, "Physiologically active substance TAN-931, etc", CA 113, 5954a (1990).
Forbes, I et al Tetrahedron Lett (41) 3965-6 1978.

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