CAS: 334-88-3; Diazomethane

1-甲基-1-硝基脲置于sodium Hydroxide体系中,用 乙醚,水 作为反应溶剂,化学反应 0.5H,反应生成 重氮甲烷
参考文献:Pde 10A Inhibitors For The Treatment Of Type Ii Diabetes
标题:Pde 10A Inhibitors For The Treatment Of Type Ii Diabetes
摘要:揭示了用于治疗2型糖尿病的化合物,组合物和方法.这些化合物由以下式(i)表示: 其中r1,R2,L和q在此处定义.

专利信息

专利号:EP-4092127-A1
优先权日:2021-05-18
标题:Enzyme-catalytic method for the direct stereoselective synthesis of gamma-(acyloxy) carboxylic acids
发明人：PARVE JAAN; KUDRJASHOVA MARINA; GATHERGOOD NICHOLAS; PARVE OMAR
权利人:TALLINN UNIV OF TECHNOLOGY
摘要:The present invention is a method for the stereoselective straightforward synthesis of gamma-acyloxy carboxylic acids of novel structure starting from racemic gamma-hydroxy carboxylic acid salts that are obtained by alkaline hydrolysis of the racemic gamma-lactones. The salt is acylated by enzyme catalysis in an organic solvent containing an acyl donor and an immobilised lipase, on stirring at room temperature (ca 20 °C) until reaching the conversion rate required. After that, the reaction mixture is acidified and extracted and the product treated with catalytic amount of para-toluenesulfonic acid in toluene during the time required for the relactonisation of the unreacted salt enantiomer. Thereafter, the target gamma-acyloxy carboxylic acid formed from one enantiomer of the starting compound and relactonised gamma-lactone formed from the other, unreacted enantiomer of the starting compound are isolated using a routine separation method, such as distillation, extraction with NaHCO3 water solution followed by acidification or column chromatography.

专利号:US-11548898-B2
优先权日:2017-07-06
标题 :Synthesis of halichondrins
发明人：KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI
权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD
摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).

专利号:US-7247752-B2
优先权日:2004-10-01
标 题 :Methods for the synthesis of astaxanthin
发明人：LOCKWOOD SAMUEL F; TANG PENG CHO; NADOLSKI GEOFF; JACKSON HENRY L; FANG ZHIQIANG; DU YISHU; YANG MIN; GEISS WILLIAM; WILLIAMS RICHARD; BURDICK DAVID
权利人:CARDAX PHARMACEUTICALS INC
摘要:A method used for synthesizing intermediates for use in the synthesis of carotenoids and carotenoid analogs, and/or carotenoid derivatives. In some embodiments, the invention includes methods for synthesizing optically active intermediates useful for the synthesis of optically active carotenoids. Synthesis of optically active carotenoids, in one embodiment, may be accomplished by forming an optically active dihydroxy intermediate from ketoisopherone. The optically active dihydroxy intermediate may be converted into optically active astaxanthin derivatives.

专利号:US-4399069-A
优先权日:1980-10-12
标题:Process for an enantioselective synthesis of optically active 14-oxo-E-homo-eburnane derivatives
发明人：SZANTAY CSABA; SZABO LAJOS; KALAUS GYORGY; SAPI JANOS; KREIDL JANOS; FARKAS NEE KIRJAK MARIA; NEMES ANDRAS; CIBULA LASZLO
权利人:RICHTER GEDEON VEGYESZET
摘要:The invention relates to a new enantioselective synthesis for the preparation of optically active 14-oxo-E-homo-eburnane derivatives of the formula (Ia) ##STR1## wherein R 1 is alkyl having from 1 to 4 carbon atom. In the synthesis optically active 6-alkoxycarbonylhexahydroindoloquinolizinium salts are employed as starting materials, which contain a center of chirality at the site of attachment of the carboxyl group. This center of chirality preserves the optical activity of the optically active tryptophan ester from which this compound has been prepared until a new center of chirality is formed in the molecule in a configuration corresponding to the desired end product. The carboxyl group, which is not needed in the end product and only serves to preserving the optical activity can then be eliminated. n Compounds of the formula (Ia) are known in the art and may be used in the synthesis of (+)-vincamine and (+)-apovincaminic acid ethylester.

专利号:US-11479577-B2
优先权日:2016-05-18
标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
发明人：WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS
权利人:NZP UK LTD
摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

专利号:US-6479549-B2
优先权日:2000-02-28
标 题:Carnosic acid derivatives for promoting synthesis of nerve growth factor
发明人：KOSAKA KUNIO; MIYAZAKI TOSHITSUGU; YOKOI TOSHIO
权利人:NAGASE & CO LTD
摘要:A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.