METHOD FOR PRODUCING RACEMIC OR OPTICALLY-ACTIVE HETEROCYCLIC COMPOUND OR ITS PHARMACEUTICALLY ACCEPTABLE ACID-ADDITIVE SALTS OR PHARMACEUTICALLY ACCEPTABLE CATION SALTS WHEN COMPOUND CONTAINS CARBOXYGROUP

摘要

(A) Bicyclic cpds. of formula (I) and their salts are new; where n = 0 or 1; m = 0-3; X = CH2, O, S, SO, SO2, NH or 1-4C alkylimino; X1 = CH2, O, S, SO or SO2; Y+Y1 = O, or Y = H and Y1 = OH or in-vivo hydrolysable acyloxy; Z = CH2, CHMe, CH2CH2 or CH2CH2CH2; Z1 = CH or N; R = 2-, 3- or 4-pyridyl, 2-, 3-, 4- or 8-quinolyl, 1-, 3- or 4-isoquinolyl, etc , , all opt. mono- or disubstd. R1 = a C-bonded phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, pyridazinyl, cinnolinyl, phthalazinyl, pyrimidinyl, naphthyridinyl, pyrrolyl, N-R11-pyrrolyl,, indolyl, N-R11-indolyl, isoindolyl, N-R11-isoindolyl, indolizinyl, pyrazolyl, 1-R11-pyrazolyl, indazolyl, 1-R11-1H-indazolyl, 2-R11-2H-indazolyl, imidazolyl, 1-R11-imidazolyl, benzimidazolyl, 1-R11-benzimidazolyl, furyl, benzofuranyl, isobenzofuranyl, oxazolyl, benzoxazolyl, isoxazolyl, benzo(c)isoxazolyl, benzo(d)isoxazolyl, thienyl, benzothiophenyl, isobenzothienyl, thiazolyl, benzothiazolyl, isothiazolyl, benzo(c)isothiazolyl or benzo(d)isothiazolyl gp., or may be 1-pyrrolyl, 1-indolyl, 2-isoindolyl, 1-pyrazolyl, 1(1H)-indozolyl, 2(2H)-indazolyl, 1-imidazolyl or 1-benzimidazolyl when X1 = CH2 or m is at least 2, where R1 is opt. mono- or disubstd. R1 and R11 = 1-4C alkyl. (B) Intermediates of formula (II) and (III) are also new: where Y2 + Y3 = O, or Y2=H and Y3 = OH; Ra = OH or benzyloxy; Rb+Rc = hydroxymethylene or diazo, or Rb = H and Rc = Br; Rb = phenyl or R.