专利号:US-8283476-B2 优先权日:2007-06-26 标 题:Transition metal catalyzed synthesis of 2H-indazoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS 权利人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.
专利号:US-8026375-B2 优先权日:2007-04-13 标题:Transition metal catalyzed synthesis of N-aminoindoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; RKYEK OMAR; URMANN MATTHIAS; ALONSO JORGE 权利人:SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:US-8188282-B2 优先权日:2006-07-15 标 题:Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS; SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-8487109-B2 优先权日:2007-07-03 标题:Process for the palladium-catalyzed coupling of terminal alkynes with aryl tosylates 发明人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; URMANN MATTHIAS; HALLAND NIS; ALONSO JORGE 权利人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; URMANN MATTHIAS; HALLAND NIS; ALONSO JORGE; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), n nwherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
专利号:US-8420812-B2 优先权日:2007-07-03 标题:Process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates 发明人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; URMANN MATTHIAS; HALLAND NIS 权利人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; URMANN MATTHIAS; HALLAND NIS; SANOFI SA 摘要:A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates n The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), n nwherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.