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Papaverine 1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-3.4-dihydroisoquinoline hydr°Chloride (3,4-Dimethoxyphenyl)acetic acid 2-(3,4-dimethoxyphenyl)-ethylamineBis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxyis°Chinolin-2-oxid] papaveraldine papaverinol Demethyl-5 formyl-5 tetrahydro-1,2,3,4 ellipticine 合成工艺路线路线简述
- 合成目标产物 Papaverine Hydrochloride 主要起始原料 1-(3,4-Dimethoxybenzyl)-3,4-Dihydro-6,7-Dimethoxyisoquinolinium Chloride
- (文献来源)合成步骤主要原料 1-(3,4-Dimethoxybenzyl)-3,4-Dihydro-6,7-Dimethoxyisoquinolinium Chloride
罂粟碱置于盐酸体系中,用 水,异丙醇 作为反应溶剂,化学反应生成 盐酸罂粟碱
参考文献:Green Technology For Salt Formation: Slurry Reactive Crystallization Studies For Papaverine Hcl And 1:1 Haloperidol-maleic Acid Salt
标题:Green Technology For Salt Formation: Slurry Reactive Crystallization Studies For Papaverine Hcl And 1:1 Haloperidol-maleic Acid Salt
摘要:盐酸罂粟碱通过悬浮反应结晶法成功制备,使用异丙醇(ipa)在25oc下进行,固液比为0.19 G/ml,老化时间为8小时,产率为82.0 W/w %,晶体尺寸为200-400 μm,熔化焓值为154.5 J/g.罂粟碱在ipa中溶解性差,而盐酸罂粟碱在含水的ipa中溶解性较好,使得盐酸罂粟碱的均相成核占主导地位.盐酸罂粟碱的晶体尺寸和结晶度随时间和温度变化.然而,1:1的氟哌啶醇-马来酸盐水合物也通过悬浮反应结晶法成功制备,使用水在25oc下进行,固液比为0.18 G/ml,老化时间为8小时,产率为82.0 W/w %,晶体尺寸为500-1000 μm,熔化焓值为84.9 J/g.氟哌啶醇和1:1的氟哌啶醇-马来酸盐水合物在水中的溶解性差,使得1:1的氟哌啶醇-马来酸盐水合物的异相成核占主导地位.1:1的氟哌啶醇-马来酸盐水合物的晶体尺寸和结晶度对时间和温度的敏感性降低.与研磨,冷却溶液反应结晶和冷却溶液再结晶相比,悬浮反应结晶是一种简单,稳健,直接,恒温低,溶剂体积小且环境友好的过程,能够获得相当的产率,粒度分布和结晶度.此外,悬浮反应结晶中使用不良溶剂使得母液可以在不显著损失产率和结晶度的情况下回收,最多可达三个循环.
DOI:10.1021/acs.Cgd.9B00098
海关参考信息
- 2902300000-甲苯
2905110000-甲醇
2907210001-间苯二酚
2933310010-吡啶 - 💡 提示:海关信息按照顺序优先匹配,如需确认的海关信息,请参考相关资料。
- 详情请参考:📖 海关编码查询和海关进出口税则
专利信息
专利号:US-2003050305-A1
优先权日:2000-05-22
标题:Thromboxane inhibitors, compositions and methods of use
发明人:TEJADA INIGO SAENZ DE
摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.
专利号:US-7772278-B2
优先权日:1999-03-01
标 题:Nitrosated and nitrosylated prostaglandins, compositions and methods of use
发明人:GARVEY DAVID S; GASTON RICKY D; LETTS L GORDON; DE TEJADA INIGO SAENZ; TAM SANG WILLIAM; WORCEL MANUEL
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, 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 vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E 1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.
专利号:US-2007010581-A1
优先权日:2002-11-29
标 题 :Use of 2,5-dihydroxybenzenesulfonic compounds for the treatment of disorders based on an impairment of no production and/or of regulation of edhf function
发明人:ESTEVE-SOLER JOSE; SAENZ DE TEJADA-GORMAN INIGO; ANGULO-FRUTOS JAVIER
权利人:ESTEVE-SOLER JOSE; SAENZ DE TEJADA-GORMAN INIGO; ANGULO-FRUTOS JAVIER
摘要:The present invention relates to the use of 2,5-dihydroxybenzenesulfonic compounds for the manufacture of medicament for the regulation of nitric oxide (NO) synthesis and/or the regulation of EDHF (Endothelium-derived-Hyperpolarizing-Factor) in the endothelium of humans or animals, whereby the medicament is administered in a daily dose of the 2,5-dihydroxybenzenesulfonic compounds of formula I of <500 mg.
专利号:US-6339160-B1
优先权日:1997-07-17
标题:Metalloproteinase inhibitors, their therapeutic use and process for the production of the starting compound in the synthesis thereof
发明人:POLITI VINCENZO; GAVUZZO ENRICO; GALLINA CARLO; STAZIO GIOVANNI DI; D ALESSIO SILVANA; SELLA ANTONIO; PIAZZA CINZIA; GIORDANO CESARE; GORINI BARBARA; PANINI GABRIELLA; PARADISI MARIO PAGLIALUNGA; CIRILLI MAURIZIO; POCHETTI GIORGIO; MAZZA FERNANDO
权利人:POLIFARMA SPA; CONSIGLIO NAZIONALE RICERCHE
摘要:Objects of the present invention are compounds of a peptido-mimetic character having the capacity of acting as inhibitors of metalloproteinases produced by venom of snake, and of other metalloproteinases of human origin which have been put in relation with various pathologies in man, including tumoral growth and metastatization, aterosclerosis, multiple sclerosis, Alzheimer's disease, osteoporosis, hypertension, rheumatoid arthritis and other inflammatory diseases. n Object of the present invention is also the procedure for the production of diethylester of (1)-phosphotryptophan, as an initial product necessary to synthesize all compounds mentioned above.
专利号:SA-109300046-B1
优先权日:2008-01-22
标题:Synthesis of herbicide clodinafob propragil and metsulfuron methyl
专利号:US-7625883-B1
优先权日:2000-11-07
标题 :Glycerophosphoinositol derivatives as modulators of cytosolic A2 phospholipase
发明人:CORDA DANIELA; DAL TOSO ROBERTO; BONVENTO GIOVANNA; MARCOLONGO GABRIELE; DAL MONTE RENZO
权利人:I R B ISTITUTO DI RICERCHE BIO
摘要:Optionally O-substituted glycero-phosphoinositol derivatives, their analogues and their salts wherein the substitutents: R′1, R′2, R2, R3, R4, R5, R6 have the described meaning, their synthesis and their pharmacological effect as modulators of the activation or over-stimulation of cPLA2.