Intermediates for the preparation of a carboxylic acid

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

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540579, 544349, 544384, A61K24118, A61K47104, A61K48704, A61K48714

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active

046970169

ABSTRACT:
The invention relates to a novel process for the preparation of the optically pure 2S- or 2R-indolinecarboxylic acid of the formula ##STR1## and salts thereof. The process comprises forming the heterocyclic 5-membered ring in formula I from an open chain precursor by diastereoselective cyclization.

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A. Padwa (Editor), Organic Photochemistry, vol. 6, (1983), pp. 16, 17, 26, 32 and 38, Dekker Inc. NY, AD601A1.
Schultz, et al., Synthesis of Functionalized, Indolines, Tetrahedron 36, 1757 (1980).
Bycroft et al., Asymmetric Synthesis of .alpha.-Amino Acids, JCS Chem. Comm. 1975, 988.
Stanton et al., J. Med. Chem., 26, 1267 (1983), Bicycl Acid Derivatives.
Yoshimara et al., Bull. Chem. Soc. Japan, 46,2850-2853 (1973).
Official Gazette Abstract for U.S. Pat. No. 4,485,241, (Nov. 27, 1984).

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