CAS: 116649-85-5; (R)-3-(3-(4-Fluorophenylsulfonamido)-3,4-Dihydro-1H-Carbazol-9(2H)-yl)Propanoic Acid

上下游产品

CAS号118699-38-0 (R)-N-[9-(2-cya... | CAS号51145-61-0 1,2,4,9-四氢咔唑-3-酮 | CAS号4746-97-8 1,4-环己二酮单乙二醇缩酮 | CAS号128432-38-2 (+/-)-2,3,4,9-t... | CAS号100-63-0 苯肼 | CAS号54621-12-4 5-oxo-tetrahydr... | CAS号116650-33-0 (R)-3-氨基-1,2,3,... | CAS号1374648-14-2 (S)-(-)-2,3,4,9... | CAS号1374648-17-5 (S)-2,3,4,9-tet...

(S)-(-)-2,3,4,9-Tetrahydro-1H-Carbazol-3-Ol置于4-二甲氨基吡啶,Sodium Azide,水,Sodium Hydride,三乙胺,三苯基膦,Sodium Hydroxide体系中,用 二氯甲烷,二甲基亚砜,N,N-二甲基甲酰胺,异丙醇 用作溶剂,化学反应 67.08H,反应生成雷马曲班
参考文献:使用脂肪酶和氧化还原酶的不对称化学酶法合成ramatroban
标题:使用脂肪酶和氧化还原酶的不对称化学酶法合成ramatroban
摘要:首次开发了用于制备对映纯(R)-Ramatroban的化学酶促不对称路线.脂肪酶和氧化还原酶的作用已被独立研究,并且被发现是在非常温和的反应条件下生产足够的手性中间体的优秀生物催化剂.Cal-B有效地催化了(+/-)-2,3,4,9-四氢-1 H-咔唑-3-醇的拆分,该拆分被高度立体控制.另一方面,Adh-A介导的4,9-Dihydro-1 H-Carbazol-3(2 H)-提供了另一种途径获得相同的对映纯醇,该对映体先前通过脂肪酶催化的拆分获得,这是合成ramatroban的有用合成基础.(S)-2,3,4,9-四氢-1 H-咔唑-3-醇的绝对构型反转已被确定为合成路线中的关键点,优化了该过程以避免叠氮化物中间体的消旋化,通过形成相应的胺和方便地官能化环外和吲哚氮原子,最终以对映纯形式生成(R)-雷马曲班.
Doi:10.1021/jo300552V

专利信息

专利号:WO-2010078250-A1
优先权日:2008-12-30
标 题:Synthesis of (2-amino)-tetrahydrocarbazole-propanoic acid
发明人：WEI YUAN; Li tianqiao; CHI YONGXIANG; ZHU JINGYANG
权利人:CHIRAL QUEST INC; WEI YUAN; Li tianqiao; CHI YONGXIANG; ZHU JINGYANG
摘要:The present invention provides a new approach to the synthesis of 2-amino-tetrahydrocarbazole-propanoic acid, a key intermediate for the synthesis of Ramatroban. More specifically, a synthesis of 2-amino-tetrahydrocarbazole- propanoic acid which includes oxidizing an aminocyclohexanol to form an aminocyclohexanone, condensing the aminocyclohexanone to form a tetrahydrocarbazole, deprotecting the tetrahydrocarbazole to yield a racemic mixture of a tetrahydrocarbazole, resolving the racemic mixture to obtain a yield mixture with an enantiomeric excess of one enantiomer over another, alkylating the excess enantiomer to yield an alkyl ester, and hydrolyzing the alkyl ester to yield 2-amino-tetrahydrocarbazole-propanoic acid.

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-6693122-B2
优先权日:1999-05-12
标题:Nitrosated and nitrosylated potassium channel activators, compositions and methods of use
发明人：GARVEY DAVID S; SAENZ DE TEJADA INIGO
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, 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 present invention also provides novel compositions comprising at least one potassium channel activator, 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 vasoactive agent. The present 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 cardiovascular disorders, cerebrovascular disorders, hypertension, asthma, baldness, urinary incontinence, epilepsy, sleep disorders, gastrointestinal disorders, migraines, irritable bowel syndrome and sensitive skin.

专利号:US-9750749-B2
优先权日:2010-05-03
标题 :Methods of treating thyroid eye disease
发明人：PHIPPS RICHARD P; GUO NAXIN; FELDON STEVEN
权利人:PHIPPS RICHARD P; GUO NAXIN; FELDON STEVEN; UNIV ROCHESTER
摘要:The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions that includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.

专利号:US-8927485-B2
优先权日:2010-02-18
标题:Site-specific modification of proteins through chemical modification enabling protein conjugates, protein dimer formation, and stapled peptides
发明人：KRANTZ ALEXANDER; YU PENG
权利人:KRANTZ ALEXANDER; YU PENG; ADVANCED PROTEOME THERAPEUTICS INC
摘要:The present invention generally provides methods for the site-specific modification of peptides, polypeptides, and proteins, e.g., granulocyte macrophage colony-stimulating factor, human superoxide dismutase, annexin, leptin, antibodies and the like, cytokines and chemokines, at their N-termini and at sites at which unnatural aminoacids have been introduced along the protein framework. The modifications described herein can be used for the synthesis and application of the adducts in radio-labeling, molecular imaging and protein therapeutic applications, and the treatment of disorders such as rheumatoid arthritis, lupus erythematosus, psoriasis, multiple sclerosis, type-1 diabetes, Crohn's disease, and systemic sclerosis, Alzheimer disease, cancer, liver disease (e.g., alcoholic liver disease), and cachexia.

专利号:CN-107501165-B
优先权日:2017-09-22
标 题 :Asymmetric Synthesis of Chiral Tetrahydrocarbazole Derivatives