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    • 71. 发明申请
    • ALKYLATING AGENT AND 1,4-ADDITION PROCESS OF AN ALKYL GROUP ONTO AN ALPHA, BETA-UNSATURATED KETONE COMPOUND
    • 烷基化AND METHOD FOR 1,4-加成的烷基,以α,β-不饱和酮化合物
    • WO1994022878A1
    • 1994-10-13
    • PCT/EP1994001001
    • 1994-03-30
    • SCHERING AKTIENGESELLSCHAFTWESTERMANN, JürgenNICKISCH, Klaus
    • SCHERING AKTIENGESELLSCHAFT
    • C07F07/12
    • C07B37/02C07F7/12C07F7/1804C07J1/0011C07J1/0025C07J1/0059
    • An alkylating agent contains an aluminium reagent Alk3-mAlLm, in which Alk stands for a methyl, ethyl, n- or i-propyl, n-, i- or tert.-butyl, pentyl, hexyl, heptyl or octyl group, which may all also be branched, L stands for an ethoxy group, for a chlorine or bromine atom and m equals 1 or 2, as alkyl source. The alkylating agent may also contain zinc dimethyl as methyl source, as well as catalytic amounts of one or several copper-I and/or copper-II compounds and one or several silyl reagents having the general formula (III), in which R , R and R may be the same or different and stand for a straight- or branched-chain alkyl residue with 1 carbon atom, or when they have a branched chain with 3 to 10 carbon atom, an alkyl residue if required substituted by 1 to 3 chlorine atoms or by 1 to 3 straight- or branched-chain alkoxy or alkyl residues with 1 carbon atom, or when they have a branched chain with 3 to 6 carbon atoms; Z stands for a chlorine, bromine or iodine atom, cyano-, perfluoroalkylsulfonyloxi residue [(CnF2n+1SO2O-), in which n = 1, 2, 3 ou 4], the mesylate residue CH3SO2O-, the tosyl residue p-CH3-C6H4-SO2O or another leaving group. This alkylating agent is used for 1,4-adding an alkyl group onto a alpha , beta -unsaturated or to an alpha , beta -biunsaturated ketone or to a alpha , beta -unsaturated aldehyde. This alkylating agent supplies biologically active compounds in extraordinarily high yields and because the reaction medium is free from chlorinated hydrocarbons, the new alkylating agent process are characterized by their environmental compatibility.
    • 77. 发明申请
    • QUINOXALINE DERIVATES WITH AFFINITY FOR QUISQUALATE-RECEPTORS
    • 喹诺酮衍生物具有适应症的受体受体
    • WO1993008173A1
    • 1993-04-29
    • PCT/DE1992000895
    • 1992-10-25
    • SCHERING AKTIENGESELLSCHAFT
    • SCHERING AKTIENGESELLSCHAFTHUTH, AndreasSCHMIECHEN, RalphBEETZ, IlseSCHUMANN, IngridTURSKI, LechoslawLÖSCHMANN, Peter, AndreasSTEPHENS, David, NormanSEIDELMANN, DieterKRÜGER, MartinRAHTZ, DieterHÖLSCHER, Peter
    • C07D241/44
    • C07F9/650994C07D241/44
    • Quinoxaline derivates have the formula (I), in which R is C1-12-alkyl substituted by R , C2-12-alkenyl substituted by R , C2-12-alkinyl substituted by R , C3-7-cycloalkyl substituted by R , -(CH2)n-C6-12-aryl substituted by R in the aryl or alkyl residue or -(CH2)n-hetaryl substituted by R in the hetaryl or alkyl residue; R is hydrogen, C1-12-alkyl substituted by R , C2-12-alkenyl substituted by R , C2-12-alkinyl substituted by R , (CH2)n-C6-12-aryl substituted by R in the aryl or alkyl residue, or -(CH2)n-hetaryl substituted by R in the hetaryl or alkyl residue; R , R , R and R are the same or different and represent hydrogen, halogen, nitro, NR R , NHCOR , SO2R , C3-7-cycloalkyloxy, COR , cyano, CF3, C1-6-alkyl, C1-4-alkoxy or imidazole possibly substituted by cyano, C1-4-alkyl or -COO-C1-6-alkyl or R and R or R and R represent a condensated benzene ring, and R stands for -CO-R , or -PO-XY and is present once or twice in the same or a different form. Also disclosed are the preparation of these derivates and their use in medicaments.
    • 喹喔啉衍生物具有式(I),其中R 1是被R 2取代的C 1-12 - 烷基,被R 2取代的C 2-12链烯基,被R 2取代的C 2-12 - 炔基 被R 2取代的C 3-7 - 环烷基, - 被芳基或烷基残基取代的 - (CH 2)n -C 6-12芳基或被R 2取代的 - (CH 2)n - 杂芳基 在杂芳基或烷基残基中; R 4为氢,被R 2取代的C 1-12 - 烷基,被R 2取代的C2-12链烯基,被R 2取代的C2-12-炔基,(CH2)n-C6- 或在芳基或烷基残基中被R 2取代的12-芳基或在杂芳基或烷基残基中被R 2取代的 - (CH 2)n - 杂芳基; R 5,R 6,R 7和R 8相同或不同,表示氢,卤素,硝基,NR 9 R 10,NHCOR 11,SO 2 R 12, C 3-7 - 环烷氧基,COR 13,氰基,CF 3,C 1-6 - 烷基,C 1-4 - 烷氧基或咪唑,其可被氰基,C 1-4 - 烷基或-COO-C 1-6 - 烷基或R <5>和R 6或R 7和R 8表示缩合苯环,R 2表示-CO-R 3或-PO-XY,并且存在一次或两次 以相同或不同的形式。 还公开了这些衍生物的制备及其在药物中的用途。