104-15-4 + 91702-98-6 + 1738-68-7 = 81110-73-8 反应条件:1.1 Reagents: Triethylamine,Dicyclohexylcarbodiimide,1-Hydroxybenzotriazole Solvents: Chloroform,Tetrahydrofuran 标题:Process For The Synthesis Of Alpha-Substituted Acrylic Acids,And Their Application As Intermediates For Amino Acid Derivatives 参考文献:European Patent Organization]
91702-98-6 + 1738-68-7 = 81110-73-8 反应条件:1.1 Reagents: Triethylamine,1-Hydroxybenzotriazole Solvents: Dimethylformamide; 1 H,0 °C; 0 °C -> Rt; 15 H,Rt 标题:Synthesis Of Racecadotril 作者:Yuan,Zhedong; Et Al 参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2006 卷标:37(5) 页码:293-294]
5669-19-2 = 81110-73-8 [标题:Reaction Conditions 标题:Direct Access To Versatile Electrophiles Via Catalytic Oxidative Cyanation Of Alkenes 作者:Gao,De-Wei; Et Al 参考文献:Journal Of The American Chemical Society 日期:2018 卷标:140(26) 页码:8069-8073]
10387-40-3 + 1738-68-7 = 81110-73-8 反应条件:1.1 Reagents: 1,1,1,3,3,3-Hexafluoro-2-Propanol,1,8-Diazabicyclo[5.4.0]Undec-7-Ene Catalysts: 4H-1,2,4-Triazolium,1,4-Dimethyl-,Iodide (1:1) Solvents: Tetrahydrofuran; 1 H,Rt1.2 6 H,Rt1.3 12 H,65 °C1.4 Solvents: Acetonitrile; 4 H,80 °C1.5 Reagents: Hydrochloric Acid Solvents: Water 标题:Copper-Catalyzed Regioselective Iodoformylation Of Terminal Alkynes To Access Versatile Electrophiles (E)-β-Iodo-α,β-Unsaturated Aldehydes 作者:Lu,Dong; Et Al 参考文献:Organic Letters 日期:2022 卷标:24(38) 页码:6993-6998]
1738-68-7 + 88320-94-9 = 81110-73-8 反应条件:1.1 Reagents: Trimethylamine Solvents: Dichloromethane; Rt; 14 H,Rt2.1 - 标题:Co- And HCL-Free Synthesis Of Acid Chlorides From Unsaturated Hydrocarbons Via Shuttle Catalysis 作者:Fang,Xianjie; Et Al 参考文献:Nature Chemistry 日期:2017 卷标:9(11) 页码:1105-1109]
28769-48-4 = 81110-73-8 反应条件:1.1 Reagents: Sulfuric Acid Solvents: Water; Rt; 15 H,130 °C; 130 °C -> Rt2.1 - 标题:Direct Access To Versatile Electrophiles Via Catalytic Oxidative Cyanation Of Alkenes 作者:Gao,De-Wei; Et Al 参考文献:Journal Of The American Chemical Society 日期:2018 卷标:140(26) 页码:8069-8073
专利号:US-6013829-A 优先权日:1996-02-05 标 题 :Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl -3- phenyl propanoic acid, application to the synthesis of N-(mercaptoacyl) amino acid derivatives 发明人:DANVY DENIS; MONTEIL THIERRY; DUHAMEL PIERRE; DUHAMEL LUCETTE; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES; NOEL-LEFEBVRE NADINE; GROS CLAUDE; PLAQUEVENT JEAN-CHRISTOPHE 权利人:BIOPROJET SOC CIV 摘要:PCT No. PCT/FR97/00218 Sec. 371 Date Nov. 26, 1997 Sec. 102(e) Date Nov. 26, 1997 PCT Filed Feb. 4, 1997 PCT Pub. No. WO97/29086 PCT Pub. Date Aug. 14, 1997Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in: a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride; b) preparing the monoacetates (VII R) or (VII S) respectively; c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R); d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R); e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R1SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).
专利号:US-5945548-A 优先权日:1995-03-03 标题:Process for the synthesis of α-substituted acrylic acids and their application 发明人:DUHAMEL PIERRE; DUHAMEL LUCETTE; DANVY DENIS; MONTEIL THIERRY; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES 权利人:BIOPROJECT SOC CIV 摘要:Process for the synthesis of α-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-8101665-B2 优先权日:2007-12-17 标题 :Process for synthesis of tritiated and deuterated thiorphan and acetorphan 发明人:MASJEDIZADEH MOHAMMAND R; WU SHAO-YONG 权利人:MASJEDIZADEH MOHAMMAND R; WU SHAO-YONG; ROCHE PALO ALTO LLC 摘要:Methods for preparing tritium or deuterium labeled thiorphan comprising reacting a compound of formula j n nwherein m is from 1 to 5 and X is halo, with Z 2 wherein Z is tritium or deuterium, in the presence of a catalyst, to form a compound of formula kn n nwherein n is from 1 to 5, provided that n is less than or equal to m.
专利号:US-7427498-B2 优先权日:1999-02-24 标题 :Composition, methods and reagents for the synthesis of a soluble form of human PHEX 发明人:CRINE PHILIPPE; BOILEAU GUY 权利人:UNIV MONTREAL 摘要:This invention relates to a soluble form of PHEX, PHEX being a type II integral membrane glycoprotein. This enzyme is the gene product of a phosphate-regulating gene with homologies to endopeptidases on the X chromosome. To produce a soluble form of PHEX, the transmembrane anchor domain has been modified to encode a signal peptidase coding sequence. The soluble PHEX therefore comprises the active ectodomain. An inactive mutant of PHEX is also an object of this invention. Both soluble and inactive mutant forms of PHEX can be used to screen ligands to PHEX. These ligands can also be used as substrates or inhibitors of PHEX. PHEX being phosphaturic, an inhibitor thereof will be used to treat phosphaturia and/or hypophosphatemia. On the opposite, a substrate for PHEX or PHEX itself can be used to treat hyperphosphatemia.
专利号:WO-2009077386-A1 优先权日:2007-12-17 标 题:Process for synthesis of tritiated and deuterated thiorphan and acetorphan
1: Said R, Arafat B, Arafat T. Quantitation of thiorphan in human plasma using LC-MS/MS and its application to a bioequivalence study. J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Aug 1;1243:124190. doi: 10.1016/j.jchromb.2024.124190. Epub 2024 Jun 15. 26(4):559-569. doi: 10.24425/pjvs.2023.148276. 118(3):616-625. doi: 10.1016/j.ijrobp.2023.09.021. Epub 2023 Sep 22. 14:1047863. doi: 10.3389/fphar.2023.1047863. 5: Le Dault E, Sicard S, Desplans J, Mayet A, Simon F, Aigle L, Savini H, Coton T, Marimoutou C; TAMIDOPEX team. A single dose of ciprofloxacin reduces the duration of diarrhea among service members deployed in Africa. Infect Dis Now. 2023 Mar;53(2):104643. doi: 10.1016/j.idnow.2023.01.003. Epub 2023 Jan 13.
合成参考文献
参考文献:10.1007/s11894-011-0208-6 摘要:Paredes-Paredes M, Flores-Figueroa J, Dupont HL. Advances in the treatment of travelers' diarrhea. Curr Gastroenterol Rep. 2011 Oct;13(5):402–7. doi: 10.1007/s11894-011-0208-6.