CAS: 6624-49-3; Isoquinoline-3-Carboxylic Acid

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203626-75-9 27104-73-0 50458-79-2

上下游产品

CAS号74163-81-8 (S)-1,2,3,4-四氢异... | CAS号67123-97-1 1,2,3,4-四氢异喹啉-3-羧酸 | CAS号1125-80-0 3-甲基异喹啉 | CAS号63-91-2 L-苯丙氨酸 | CAS号143468-70-6 (4-nitrophenyl)... | CAS号50458-79-2 3-异喹啉甲酸乙酯 | CAS号67123-97-1 1,2,3,4-四氢异喹啉-3-羧酸 | CAS号25475-67-6 3-氨基异喹啉 | CAS号50458-77-0 3-异喹啉羧酰胺

📜(R)-(+)-1,2,3,4-四氢异喹啉-3-羧酸置于ammonium Hydroxide,Recombinant Escherichia Coli Bl21 (De3) Cells Expressed D-Amino Acid Oxidase From Fusarium Solani M-0718,氧气体系中,用 水 作为反应溶剂,化学反应 24.0H,以90%的收率获得产物异喹啉-3-甲酸
参考文献:使用d-氨基酸氧化酶的(S)-1,2,3,4-四氢异喹啉羧酸的化学酶法
标题:使用d-氨基酸氧化酶的(S)-1,2,3,4-四氢异喹啉羧酸的化学酶法
摘要:光学纯的1,2,3,4-四氢异喹啉羧酸是合成天然产物和合成药物的重要组成部分.然而,由于缺少合适的氧化还原酶,外消旋的1,2,3,4-四氢异喹啉羧酸的氧化还原脱硫仍然是一个有吸引力的方法.本文中,通过基因组挖掘,利用了镰刀菌m-0718(fs Daao)的d-氨基酸氧化酶,具有广泛的底物范围和优异的对映选择性,并用于动力学拆分多个外消旋的1-3位羧基取代的四氢异喹啉以得到相应的(小号具有优异的对映体过量()-对映体ee)值(最高> 99%).通过在一锅中将fs Daao与氨硼烷结合使用,这些外消旋的羧基取代的四氢异喹啉可进行脱硝,转化率高达ee > 98%和ee > 99%.外消旋的1,2,3,4-四氢异喹啉-1-羧酸和1,2,3,4-四氢异喹啉-3-羧酸的制备规模脱硝反应也显示出非常好的分离收率(分别为82%和73%),且ee > 99%.我们的研究为合成对映体纯的1,2,3,4-四氢
DOI:10.1002/adsc.201900178

专利信息

专利号:US-8735586-B2
优先权日:2007-06-26
标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR
权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; 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 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: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-2008242861-A1
优先权日:2007-04-02
标题 :Synthesis of amino-protected cyclohexane-1,4-diyldimethanamine and its derivatives
发明人：YEN CHI-FENG; HUANG CHANG-PIN; HU CHENG-KUNG; CHOU MING-CHEN; KING CHI-HSIN RICHARD
权利人:YEN CHI-FENG; HUANG CHANG-PIN; HU CHENG-KUNG; CHOU MING-CHEN; KING CHI-HSIN RICHARD
摘要:This invention relates to methods of preparing the compounds of formula (V): n n n n n n n n n n Each variable in this formula is defined in the specification.

专利号:US-8410130-B2
优先权日:2007-11-07
标题 :Synthesis of 8H-3A-aza-cyclopenta [A ]indenes and 5,10-dihydropyrrolo[1,2-B]isoquinolines derivatives and their use as antitumor therapeutic agents
发明人：SU TSANN-LONG; CHOU TING-CHAO
权利人:SU TSANN-LONG; CHOU TING-CHAO; ACADEMIA SINICA
摘要:The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications.

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

专利号:US-2024279231-A1
优先权日:2021-05-20
标题:Map4k4 inhibitors and methods of synthesis and use thereof
发明人：AWASTHI VIBHUDUTTA; EEDA VENKATESWARARAO
权利人:UNIV OKLAHOMA
摘要:The compound DMX-5804, IUPAC name 5-(4-(2-methoxyethoxy)phenyl)-7-phenyl-3,4a,7,7a-tetrahydro-4H-pyrrolo[2,3-d]pyrimidin-4-one, is a potent and selective inhibitor of mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4). The present disclosure describes a scalable and practical synthesis process for making DMX-5804. The process (1) doesn't rely on transition metals, (2) has reduced duration of reactions, (3) is streamlined with significantly improved yields using low cost raw materials, (4) includes no microwave-assisted reactions, (5) does not require column purification, and (6) generally results in crystalized products having over a 95% purity in each step. The present disclosure also describes DMX-5804 analogs and derivatives for use in inhibiting MAP4K4, and scalable and practical processes for making such DMX-5804 analogs.