📜苯氧基丙酮,对羟基去甲麻黄碱置于sodium Cyanoborohydride,三乙胺,盐酸体系中,用 甲醇,水 用作溶剂,以54%的收率获得异舒普林 参考文献:Phenethanolamine-Derived Haptens,Immunogens And Conjugates Comprising Them And Antibodies Recognising Said Immunogenes And Conjugates 标题:Phenethanolamine-Derived Haptens,Immunogens And Conjugates Comprising Them And Antibodies Recognising Said Immunogenes And Conjugates
专利号:EP-0364340-B1 优先权日:1988-10-05 标题:Method for the synthesis of sulfonyl imides 摘要:Method for the synthesis of sulfonylimidides having the formula M((RSO2)2N)y, whrein M is a metal or an ammonium radical quaternary or not, the Rs, which may be identical or similar are organic monovalent radicals, particularly hydrocarbyles and preferably perfluorohydrocarbyles, in C1 to C12, and y is the valence of M. On the one hand, a silazane component selected amongst the silazane compounds M(((R2)3Si)2N)y or the associations of a silazane derivative A((R2)3Si)2N or a fluoride M1Fz of low cross-linking energy is reacted with, on the other hand, at least one sulfonic halogenite component consisting of a sulfonyl fluoride RSO2F or in the association of a sulfonyl chloride RSO2Cl with a fluoride M1Fz, M, R and y having the above-mentionned significations, M1 being selected amongst the Ms and being optionally identical to M, z being the valence of M1 and R2 representing an alkyl in C1 to C4. The imidides obtained for which the R2 are perfluorated radicals and M is an alkaline metal such as Li are usable in association with polyethers for the production of materials of the ionic conduction type for all solid generators in thin films.
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-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-6214847-B1 优先权日:1997-08-14 标题 :Crystalline 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone and an improved process for preparing the same 发明人:PESTI JAAN A; FORTUNAK JOSEPH M; HUHN GEORGE F; MAURIN MICHAEL; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates to processes for the synthesis of a crystalline polymorph of 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone in high purity. The product is useful in the synthesis of pharmaceutical compounds for the reduction of cholinergic system dysfunction.
专利号:WO-9003968-A1 优先权日:1988-10-05 标 题:Method for the synthesis of sulfonylimidides
专利号:EP-0364340-A1 优先权日:1988-10-05 标 题 :Method for the synthesis of sulfonyl imides
1: Erkert RS, Macallister CG. Isoxsuprine hydrochloride in the horse: a review. J Vet Pharmacol Ther. 2002 Apr;25(2):81-7. doi: 10.1046/j.1365-2885.2002.00386.x. 170:152-163. doi: 10.1016/j.jphotobiol.2017.04.007. Epub 2017 Apr 11. 38(3):291-295. doi: 10.1055/s-0039-1696720. Epub 2019 Sep 24. 24(5):987. doi: 10.3390/molecules24050987. 5: Shahraki S, Delarami HS, Saeidifar M, Nejat R. Catalytic activity and structural changes of catalase in the presence of Levothyroxine and Isoxsuprine hydrochloride. Int J Biol Macromol. 2020 Jun 1;152:126-136. doi: 10.1016/j.ijbiomac.2020.02.064. Epub 2020 Feb 8. from the perspective of comparison. Int J Biol Macromol. 2018 Apr 1;109:576-588. doi: 10.1016/j.ijbiomac.2017.12.117. Epub 2017 Dec 21.
合成参考文献
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