CAS: 146-48-5; Yohimbine

上下游产品

yohimbinic acid corynanthine 3α-15α-20β-17α-hydroxylyohimbine-16α-carboxylic acid methyl ester (+)-3,14-didehydroyohimbine yohimbinic acid (R)-2-methyl-2-(2,4,5-trichlorophenoxy)acetic acid Indole-2-carboxylic acid

17β-Hydroxy-18,19-Didehydroyohimbane置于palladium On Activated Charcoal 甲醇,六甲基磷酰三胺,四丙基高钌酸铵,4 A Molecular Sieve,氢气,L-Selectride,Potassium Carbonate,N-甲基吗啉氧化物,Lithium Diisopropyl Amide体系中,用 四氢呋喃,甲醇,二氯甲烷 用作溶剂,-78.0~25.0 °C,101.33 Kpa 条件下,反应 11.75H,反应生成育亨宾
参考文献:Symmetry-Driven Synthesis Of Indole Alkaloids: Asymmetric Total Syntheses Of (+)-Yohimbine,(-)-Yohimbone,(-)-Yohimbane,And (+)-Alloyohimbane
标题:Symmetry-Driven Synthesis Of Indole Alkaloids: Asymmetric Total Syntheses Of (+)-Yohimbine,(-)-Yohimbone,(-)-Yohimbane,And (+)-Alloyohimbane
摘要:Total Asymmetric Syntheses Of The Target Alkaloids Are Reported. The Syntheses Involve The Preparation Of Enantiomerically Pure (S,S)-1,3,3A,4,7,7A-Hexahydro-2(H)-Inden-2-One 7 And Its Meso Isomer 5. Each Ketone Is Then Converted Into A Ring-Expanded Lactam Using An Oxaziridine Synthesis/rearrangement Protocol. The Applications Of Bischler-Napieralski Ring Constructions Along With Appropriate Functional Group Transformations Afford Enantiomerically Enriched Alloyohimbane Or Yohimbane From The Meso-Or C-2-Symmetric Ketones,Respectively. A Cis-5,6-Diacetoxy Compound (18) Derived From The (S,S)-Ketone Served As The Starting Material For The Total Syntheses Of The More Highly Functionalized Alkaloids. Accordingly,A Site-Specific Insertion Of The Indole-Containing Side Chain Was Accomplished Via Stereoselective Formation Of An Oxaziridine Followed By Its Stereospecific Rearrangement. The Selectivity Of This Sequence Allowed For The Differentiation Of Alcohols At C-17 And C-18 (Yohimbine Numbering) And The Synthesis Of Delta 18,19-Yohimbone. This Alpha,Beta-Unsaturated Ketone Was Converted Into Either (-)-Yohimbone Or (+)-Yohimbine Using Standard Chemistry.
Doi:10.1021/ja00099A019

专利信息

专利号:US-4105651-A
优先权日:1976-03-15
标 题:Purification of enkephalin, an endogenous composition in the human body and synthesis of same
发明人：HUGHES JOHN
权利人:US HEALTH EDUCATION & WELFARE
摘要:The purification of an endogenous composition isolated from mammalian brain tissue and termed enkephalin ('in the head'). Enkephalin is recovered from brain tissue by acetone solution and purified by means of column and thin layer chromatography. The composition which is a mixture of two pentapeptides, namely, (a) H-Tyr-Gly-Gly-Phe-Met-OH and (b) H-Tyr-Gly-Gly-Phe-Leu-OH wherein the ratio of a:b is from 3:1 to 4:1 has been found to be a non-addictive narcotic and an opiate agonist. n The synthesis of the pentapeptide composition from the known structure above is accomplished by conventional solution techniques of protection of the amino groups, such as t-butyloxycarbonyl, benzyloxycarbonyl, and t-amyloxycarbonyl, or the solid phase peptide synthesis of R. Bruce Merrifield using a polymeric support and the same or similar amine protecting groups.

专利号:US-11912647-B2
优先权日:2020-05-22
标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation
发明人：CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS
权利人:UNIV GEORGIA
摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2025092433-A1
优先权日:2023-09-20
标 题:Polypeptides for use in the synthesis of kratom alkaloids
发明人：CASARETTO JOSE; AKTAR TARIQ A; ROTHSTEIN STEVEN; SOUBEYRAND ERIC
权利人:MITRADYNE CORP
摘要:Described herein are polypeptides encoding enzymes for the synthesis of monoterpene indole alkaloids. For example, the polypeptide comprises or consists of the sequence of SEQ ID NO: 1-68, or a variant thereof having at least 80% sequence identity to SEQ ID NO: 1-68, or a fragment of the polypeptide, or the variant thereof.

专利号:US-9765027-B2
优先权日:2014-08-22
标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation
发明人：VARDANYAN RUBEN S; HRUBY VICTOR J
权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA
摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.

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.