4-(2-chloroethyl)-1H-imidazole4-cyanomethylimidazolemon°Cloridrato di 2-(2-tiono-4-imidazolin-4-il)etilaminaD,L-histidine[2-(1H-Imidazol-4-yl)-ethyl]-dimethyl-aminepyridine4,5,6,7-tetrahydro-1H-imidazo4,5-cpyridine5,6,7,8-tetrahydro-5-oxoimidazo[1,5-c]pyrimidine(3)H-imidazol-4-yl)-ethylamino]-ethyl}-phenol4-{2-[2-(1(3)H-imidazol-4-yl)-ethylamino]-ethyl}-phenol
专利号:US-5919969-A 优先权日:1996-06-05 标 题 :Synthesis of yellow couplers 发明人:CRAWLEY MICHAEL W 权利人:EASTMAN KODAK CO 摘要:The invention provides a method of synthesis of a image-dye forming coupler of formula (I) wherein X is a substituent linked to the coupler by an atom of oxygen, sulfur or nitrogen R1 is an alkyl or aryl group, R2 is a hydrogen atom or an alkyl group; R3 to R7 are the same or different and selected from a hydrogen atom and substituent groups; which method comprises the reaction of a compound of formula (II) wherein R and R1 are the same or different and are as defined above for R1 and X is as defined above with a compound of formula (III) wherein R2 to R7 are as defined above, in the presence of an inert organic solvent.
专利号:WO-2025136243-A1 优先权日:2023-12-20 标题:Mechanochemical synthesis of histamine h1-receptor antagonists 发明人:AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA 权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT 摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.
专利号:US-6620942-B2 优先权日:1998-12-23 标题 :Synthesis of histamine dihydrochloride 发明人:YEH WEN-LUNG; ANTCZAK CASIMIR; MCGOLRICK JEFFRY DAVID; ROTH MICHAEL JOSEPH; WRONA MARK 权利人:MAXIM PHARMACEUTICALS 摘要:The invention disclosed herein relates to the preparation of pharmaceutical grades of histamine dihydrochloride using a two step non-enzymatic synthetic method. The invention disclosed herein describes the synthesis of histamine dihydrochloride by the non-enzymatic decarboxylation of histidine and the step-wise conversion of the decarboxylated product to the dihydrochloride salt form. The invention disclosed herein considers a final product of histamine dihydrochloride containing less than each of the following: 0.8% L -histidine HCl monohydrate, 0.1% individual chromatographic impurities, and 2% total impurities, to be acceptable for pharmaceutical use.
专利号:US-6803468-B2 优先权日:2000-08-29 标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine 发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR 权利人:RANBAXY LAB LTD 摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).
专利号:US-6909010-B2 优先权日:2001-04-11 标题:Facile synthesis of symmetric esters of alkylenebisphosphonic acids 发明人:HERLINGER ALBERT W; STEPINSKI DOMINIQUE C 权利人:UNIV LOYOLA CHICAGO 摘要:A facile synthesis of symmetric esters of C 1 -C 10 alkylenebisphopsphonic acids is disclosed in which a C 1 -C 10 alkylenebis(phosphonic dichloride) is reacted with an alcohol in the presence of a catalytic amount of 1H-tetrazole and a base in an aprotic solvent to form a first reaction mixture. The first reaction mixture is maintained for a time period sufficient to form a C 1 -C 10 alkylenebis(chloro ester phosphonate) that is reacted under basic conditions with an excess of a hydroxylated compound to form a second reaction mixture that is itself maintained for a time period sufficient to form a C 1 -C 10 alkylenebis(ester phosphonate) partial ester, homoleptic tetraester or mixed tetraester. The material so formed can be recovered or used as is.
专利号:US-6642376-B2 优先权日:2001-04-30 标 题 :Rational synthesis of heteroleptic lanthanide sandwich coordination complexes 发明人:LINDSEY JONATHAN S; GROSS THORALF 权利人:UNIV NORTH CAROLINA STATE 摘要:A half-sandwich coordination complex, useful for the synthesis of triple-decker sandwich coordination compounds, is produced by reacting a precursor complex of the formula XM(R 1 ) 2 wherein X is a halogen, M is a metal, and R 1 is an amide, with a free base porphyrinic macrocycle to produce said half-sandwich complex. The half-sandwich coordination complex can be used to make a triple-decker sandwich coordination compound by reacting a half-sandwich coordination complex as described above with a double-decker sandwich coordination compound.
[参考文献]: Chiheng Chu, Et Al. Enhanced Indirect Photochemical Transformation Of Histidine And Histamine Through Association With Chromophoric Dissolved Organic Matter. Environ Sci Technol. 2015 May 5;49(9):5511-9. [参考文献]: Hiroki Kaneko, Et Al. Histamine H4 Receptor As A New Therapeutic Target For Choroidal Neovascularization In Age-Related Macular Degeneration. Br J Pharmacol. 2014 Aug;171(15):3754-63. [参考文献]: Kenji Maeda, Et Al. Brexpiprazole I: In Vitro And In Vivo Characterization Of A Novel Serotonin-Dopamine Activity Modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604. [参考文献]: Kristin Bjornsdottir-Butler, Et Al. Prevalence And Characterization Of High Histamine-Producing Bacteria In Gulf Of Mexico Fish Species. J Food Prot. 2015 Jul;78(7):1335-42. [参考文献]: Lin Lin, Et Al. Histamine Inhibits Differentiation Of Skin Fibroblasts Into Myofibroblasts. Biochem Biophys Res Commun. 2015 Jul 31;463(3):434-9.
合成参考文献
参考文献:10.1113/expphysiol.2009.051102 摘要:Flores CA, Cid LP, Sepúlveda FV. Strain-dependent differences in electrogenic secretion of electrolytes across mouse colon epithelium. Exp Physiol. 2010 Jun;95(6):686–98. doi: 10.1113/expphysiol.2009.051102. 摘要:Law R, Maltepe C, Bozzo P, Einarson A. Treatment of heartburn and acid reflux associated with nausea and vomiting during pregnancy. Can Fam Physician. 2010 Feb;56(2):143–4. 参考文献:10.1159/000089026 摘要:Walker T, von Komorowski G, Scheurlen W, Dorn-Beineke A, Back W, Bayerl C. Neonatal mastocytosis with pachydermic bullous skin without c-Kit 816 mutation. Dermatology. 2006;212(1):70–2. doi: 10.1159/000089026. 参考文献:10.1159/000089030 摘要:Kawada K, Maeda N, Kobayashi S, Sowa J, Tsuruta D, Kawada N. Injection site with generalized rash caused by pegylated interferon alpha 2a injection. Dermatology. 2006;212(1):82–3. doi: 10.1159/000089030. 参考文献:10.1159/000089035 摘要:Pitarch G, Torrijos A, Martínez-Menchón T, Sánchez-Carazo JL, Fortea JM. Familial aquagenic urticaria and bernard-soulier syndrome. Dermatology. 2006;212(1):96–7. doi: 10.1159/000089035.