CAS: 154-86-9; Dl-Phenylephrine (Hydrochloride)

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1477-63-0 939-38-8 154-86-9

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CAS号61-76-7 盐酸去氧肾上腺素 | CAS号33543-61-2 3-[2-(methylami... | CAS号61-76-7 盐酸去氧肾上腺素

📜1-(3-羟基苯基)-2-[甲基(苯甲基)氨基]乙酮盐酸盐置于盐酸,Palladium On Carbon,氢气体系中,用 甲醇,水 用作溶剂,45.0 °C,1.0 Mpa 条件下,以80.51 %的收率获得去氧肾上腺素
参考文献:一种盐酸去氧肾上腺素原料药中杂质的制备方法
标题:一种盐酸去氧肾上腺素原料药中杂质的制备方法
摘要:本发明涉及药物化学技术领域,具体涉及盐酸去氧肾上腺素原料药中杂质的制备方法.本发明提供一种盐酸去氧肾上腺素原料药中杂质的制备方法,包括以间羟基苯乙酮为原料,经溴素溴化,得到2‑溴‑1‑(3‑羟基苯基)乙烷‑1‑酮溶液(中间体1),中间体1再与n‑甲基苄胺胺化,酸化,得到1‑(3‑羟基苯基)‑2‑[甲基(苯基甲基)氨基]乙酮盐酸盐(中间体2),中间体2后经氢化还原,脱去苄基,得到目标产物杂质c.本发明方法简单高效,收率较高,制备得到的杂质可为盐酸去氧肾上腺素原料药的质量分析提供对照品.杂质c的化学结构式为:#imgabs0#

专利信息

专利号:US-6436997-B1
优先权日:1998-06-01
标题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension
发明人：DE TEJADA INIGO SAENZ
权利人:NITROMED INC
摘要:The present invention provides methods of promoting synthesis of nitric oxide or endothelium-derived relaxing factor (EDRF) in hypoxic mammalian tissues by administering at least one N-hydroxyguanidine compound that is a substrate of nitric oxide synthase, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides methods of promoting vasorelaxation and treating sexual dysfunctions in patients by administering at least one N-hydroxyguanidine compound that is a substrate for nitric oxide synthase, and, optionally, at least one vasoactive agent and/or thromboxane A2 receptor antagonist. The present invention also provides methods for treating clinical conditions resulting from hypoxic conditions such as pulmonary disease, cardiovascular disorders, circulatory hypoxia, specific organ hypoxia, localized hypoxia, edema, central nervous system disorders, memory loss, or arterial disease. The present invention also provides methods for treating clinical conditions resulting from an abnormally high level of arginase activity, such as, heart disease, systemic hypertension, pulmonary hypertension, sexual dysfunction, autoimmune disease, chronic renal failure and cerebral vasospasm. The present invention also provides methods for treating clinical conditions associated with a deficient nitric oxide pathway by administering at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides pharmaceutical compositions comprising at least one N-hydroxyguanidine compound, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists.

专利号:US-5094782-A
优先权日:1990-12-24
标 题:Synthesis of capsacin derivatives and their use as an analgesic drug and vessel dilation drug
发明人：CHEN ING-JUN; YEH JWU-LAI
权利人:NAT SCIENCE COUNCIL REPUBLIC CHINA
摘要:Nonanoyl vanillylamide succinate was synthesized from synthetic capsaicin (nonanoyl vanillylamide) and succinic anhydride. The antinociceptive and cardiovascular effects of nonanoyl vanillylamide and its derivatives were investigated. We found that nonanoyl vanillylamide and nonanoyl vanillylamide succinate strongly inhibited the writhing response, led to the vascular smooth muscle relaxation, produces bradycardia and a fall of blood pressure. The potency of nonanoyl vanillylamide succinate was found to be slight greater than that of nonanoyl vanillylamide, when compared with the same molar dose/kg of their administrations.

专利号:US-4158005-A
优先权日:1975-02-10
标题:Intermediates useful in the synthesis of optically active m-acyloxy-α-[(methylamino)methyl]benzyl alcohols
发明人：BODOR NICOLAE S; YUAN SUN-SHINE
权利人:INTERX RESEARCH CORP
摘要:Optically and therapeutically active compounds of the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C 1 -C 5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##STR2## WHEREIN R is as defined above and R 3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are prepared optically active m-hydroxy-α-[methylamino)methyl]benzyl alcohol (phenylephrine). n The compounds prepared by the process of this invention find therapeutic application to warm-blooded animals (e.g., humans) in the management of asthma, nasal congestion and as decongestants, vasoconstrictors, mydriatic agents, and anti-glaucomatous agents in the practice of ophthalmology. n Upon administration, these compounds will enzymatically 'cleave,' thus releasing optically active phenylephrine (m-hydroxy-α-[(methylamino)methyl]benzyl alcohol, the therapeutically active moiety thereof.

专利号:US-4028368-A
优先权日:1975-02-10
标 题:Novel intermediates useful in the synthesis of optically active m-acyloxy-α-[(methylamino)methyl]benzyl alcohols
发明人：BODOR NICOLAE S; YUAN SUN-SHINE
权利人:INTERX RESEARCH CORP
摘要:Optically and therapeutically active compounds of the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C 1 -C 5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##STR2## group, wherein R is as defined above and R 3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are prepared using optically active m-hydroxy-α-[(methylamino)methyl]benzyl alcohol (phenylephrine).

专利号:US-4174450-A
优先权日:1975-02-10
标 题:Intermediates useful in the preparation of optically and therapeutically active-m-acyloxy-(methyl-amino) methyl benzyl alcohols
发明人：BODOR NICOLAE S; YUAN SUN-SHINE
权利人:INTERX RESEARCH CORP
摘要:This invention deals with chemical intermediates having the formula ##STR1## wherein R 1 and R 2 together with the carbon atom to which they are attached form a single hetero atom member selected from the group consisting of a five-to seven-membered heterocycle containing one hetero-N-atom and a N-substituted five-to seven-membered heterocycle containing an hetero-N-atom whose substituent is C 1 -C 2 alkyl. These compounds are useful in the synthesis of compounds having a variety of uses as pharmaceuticals.

专利号:US-8617854-B2
优先权日:2008-09-17
标题 :Method for producing L-phenylephrine using an alcohol dehydrogenase of Aromatoleum aromaticum EBN1 (Azoarcus sp. EBN1)
发明人：BREUER MICHAEL; PLETSCH ANDREAS; HAUER BERNHARD; SIEGEL WOLFGANG
权利人:BREUER MICHAEL; PLETSCH ANDREAS; HAUER BERNHARD; SIEGEL WOLFGANG; BASF SE
摘要:The present invention relates to a multi-stage process for producing substituted, optically active alcohols, comprising an enzyme-catalyzed synthesis step, in particular a synthesis step which is catalyzed by an alcohol dehydrogenase. The inventive method is particularly suitable for producing phenylephrine, i.e. 3-[(1R)-1-hydroxy-2-methylamino-ethyl]-phenol.