| 摘要 |
<p>EP--85840 A s-Triazolo(3,4-a)phthalazine derivs. of formula (I) are new. In (I) R is (a) H, OH or 1-6C alkyl, (b) phenyl opt. substd. by 1-3 of 1-6C alkyl, 1-6C alkoxy, Cl, F, Br, I, Ph, OH, NH2, (di)alkylamino, 2-4C alkanoylamino, piperidino, CN, NO2, CF3, COOH and CONH2, (c) 2-5C alkoxycarbonyl, Cl, SH, 1-4C alkylthio, alkylsulphinyl or alkylsulphonyl, (d) NR4R5, where R4 and R5 are H, alkenyl or alkyl opt. (di)substd. by OH, alkoxy, halogen, COOH, CN, CONH2, (di)alkylcarbamoyl, alkoxy(thio)carbonyl and/or alkylthiocarbonyl, or R4 and R5 are phenylalkyl opt. substd. as above, or NR4R5 is satd. 4- to 7-membered heterocycle opt. contg. another N, O or S heteroatom and/or substd. by 1 or 2 of alkyl, opt. substd. phenyl, OH and alkoxycarbonyl, or (e) OR6, where R6 is 1-6C alkyl opt. substd. by 1 or 2 of OH, NH2, (di)alkylamino, alkoxy, halogen, oxo, COOH, CONH2, (di)alkylcarbamoyl, alkoxy-carbonyl, alkoxythiocarbonyl and alkylthiocarbonyl or R6 is a heterocycle as defined for NR4R5, or R6 is 5-8C cycloalkyl opt. substd. by OH and/or alkoxy; R1 is halogen, OH, 1-4C alkylthio, alkylsulphinyl or alkylsulphonyl, phenyl opt. substd. above, or NR7R8 or OR9, where R7 and R8 are as defined for R4 and R5, and R9 is as defined for R6. R2 and R3 are H, halogen, 1-4C alkyl, 1-4C alkoxy or NO2; with the provisos that (a) R cannot be phenyl or 4-nitrophenyl when R2=R3=H and R1=Cl, (b) R cannot be phenyl when R1=OH, and (c) the heterocycle cannot be bonded to O via a heteroatom in heterocyclic gps. OR6 and OR9. - Intermediates of formula (III) are also new. EPAB- EP--85840 B s-Triazolo(3,4-a)phthalazine derivs. of formula (I) are new. In (I) R is (a) H, OH or 1-6C alkyl, (b) phenyl opt. substd. by 1-3 of 1-6C alkyl, 1-6C alkoxy, Cl, F, Br, I, Ph, OH, NH2, (di)alkylamino, 2-4C alkanoylamino, piperidino, CN, NO2, CF3, COOH and CONH2, (c) 2-5C alkoxycarbonyl, Cl, SH, 1-4C alkylthio, alkylsulphinyl or alkylsulphonyl, (d) NR4R5, where R4 and R5 are H, alkenyl or alkyl opt. (di)substd. by OH, alkoxy, halogen, COOH, CN, CONH2, (di)alkylcarbamoyl, alkoxy(thio)carbonyl and/or alkylthiocarbonyl, or R4 and R5 are phenylalkyl opt. substd. as above, or NR4R5 is satd. 4- to 7-membered heterocycle opt. contg. another N, O or S heteroatom and/or substd. by 1 or 2 of alkyl, opt. substd. phenyl, OH and alkoxycarbonyl, or (e) OR6, where R6 is 1-6C alkyl opt. substd. by 1 or 2 of OH, NH2, (di)alkylamino, alkoxy, halogen, oxo, COOH, CONH2, (di)alkylcarbamoyl, alkoxy-carbonyl, alkoxythiocarbonyl and alkylthiocarbonyl or R6 is a heterocycle as defined for NR4R5, or R6 is 5-8C cycloalkyl opt. substd. by OH and/or alkoxy; R1 is halogen, OH, 1-4C alkylthio, alkylsulphinyl or alkylsulphonyl, phenyl opt. substd. above, or NR7R8 or OR9, where R7 and R8 are as defined for R4 and R5, and R9 is as defined for R6. R2 and R3 are H, halogen, 1-4C alkyl, 1-4C alkoxy or NO2; with the provisos that (a) R cannot be phenyl or 4-nitrophenyl when R2=R3=H and R1=Cl, (b) R cannot be phenyl when R1=OH, and (c) the heterocycle cannot be bonded to O via a heteroatom in heterocyclic gps. OR6 and OR9. - Intermediates of formula (III) are also new. (93pp) USAB- US4788186 A s-Triazolo(3,4-a)phthalazine derivs. of formula (I) are new. R is phenyl opt. substd. by monohydroxy or 1-3 of 1-6C alkyl, 1-6C alkoxy, Cl, F, Br, phenyl, amino, (mono- or di-) 1-4C alkylamino, 2-4C alkanoylamino, piperidino, cyano, nitro, trifluoromethyl, carboxy or carbamoyl, with provisos, or R is carbo-1-4C-alkoxy, Cl, 1-4C alkylsulphinyl, 1-4C alkylsulphonyl, -N(R4)(R5), or OR6; R1 is halogen, hydroxy, 1-4C alkylthio, 1-4C alkylsulphinyl, 1-4C alkylsulphonyl, opt. substd. phenyl, -N(R7)(R8), or OR9; R2 is H; R3 is H, halogen, 1-4C alkyl, 1-6C alkoxy or nitro with provisos; R4 and R5 are each 1-4C alkyl, 2-4C alkyl substd. by hydroxy, 1-4C alkoxy, halogen, carboxy, cyano, aminocarbonyl, mono- or di- 1-4C alkylaminocarbonyl, 1-4C alkoxycarbonyl, 1-4C alkoxythiocarbonyl, and/or 1-4C alkyl-thiocarbonyl, or R4 and R5 are each opt. substd. phenyl 1-4C alkyl or R4 and R5 together form a satd. 4-6 membered heterocyclic ring with the N to which they are attached; R6 is 1-6C alkyl substd. with 1 or 2 gps., satd. 4-6 membered ring which is azetidine, pyrrolidine, piperidine, piperazine or morpholine, each opt. substd., or R6 is opt. substd. 5-8C cycloalkyl; R7 and R8 are as R4 and R5; and R9 is as R6. Specifically claimed is e.g., 3-phenyl-6-(1-pyrrolidinyl)-1,2,4-tri azolo(3,4,-a)phthalazine.</p> |
