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:WO-2017089470-A1 优先权日:2015-11-27 标 题:Process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases 发明人:HOFMANN DAGMAR; HOFMANN JOSEFA; HEINRICH MARKUS 权利人:Friedrich-Alexander-Universität Erlangen-Nürnberg 摘要:The present invention relates to a process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases.
专利号:US-2013150622-A1 优先权日:2011-12-12 标题:Stereoselective synthesis of tapentadol and its salts 发明人:FANDRICK DANIEL ROBERT; RODRIGUEZ SONIA; YANG BING-SHIOU 权利人:BOEHRINGER INGELHEIM INT; BOEHRINGER INGELHEIM INT 摘要:A process for the synthesis of a salt of tapentadol.
专利号:WO-2008134923-A1 优先权日:2007-04-28 标题 :A preparation method of thiol derivative as side chain intermediate for synthesis of carbapenem derivative 发明人:CAI JIANPING; FAN ENHAI 权利人:ZHEJIANG NEXCHEM PHARMACEUTICA; CAI JIANPING; FAN ENHAI 摘要:A preparation method of thiol derivative as side chain intermediate for synthesis of carbapenem derivative. The method is starting with trans-4-hydroxy-L-proline derivative as starting material, following by one-pot method that 2-carbonyl group is protected, 4-hydroxy is protected and 2-postion is substituted to obtain 2-amide proline derivative, then 4-postion is substituted and 4-postion is hydrolyzed in the presence of base to obtain thiol side chain derivative as important intermediate for Meropenem. The present method is simple, without separating intermediates, with high yield and easy to operate and has advantages over the prior patent methods. It is suitable for industrial production.
专利号:WO-2013144924-A1 优先权日:2012-03-29 标 题:An improved process for the synthesis of strobilurin fungicides viz trifloxystrobin and kresoxim-methyl 发明人:KAMARAJ PASUMPON; SATAM VIJAY SHRIKANT; AJJANNA MAHALINGAPPA SRIDHARA; NANDI TAPASKUMAR; BOBADE ANNA; SHINDE RAVINDRA; NAIK PARAG; MOHITE DHANAJI; KADAM SUBHASH; HINDUPUR RAMA MOHAN; PATI HARI NARAYAN; MANE AVINASH; VADIRAJ SUPHALA GOPINATH; VENKATESH PRABHU MOODBIDRI 权利人:RALLIS INDIA LTD 摘要:The present invention relates to an improved process for the synthesis of E -isomer of compound of formula (5). It further relates to the conversion of formula (5), wherein R is H, to Intermediate (I) and subsequently to substantially pure Trifloxystrobin, compound of formula (I) in good yield.
专利号:EP-2589587-A1 优先权日:2011-11-04 标题:Synthesis of nitrogen substituted cyclopropanes 发明人:RASPARINI MARCELLO; TADDEI MAURIZIO; CINI ELENA; MINELLI COSIMA; TURNER NICHOLAS; HUGENTOBLER KATHARINA GLORIA 权利人:CHEMO IBERICA SA 摘要:The invention is about a new synthetic pathway for the preparation of enantiomerically pure nitrogen substituted cyclopropanes, in particular the trans- cyclopropanamine ( 1 ), a key intermediate in the synthesis of Ticagrelor:n n The invention also relates to the processes for preparing said compounds or their salts and the use of said compounds as intermediates in preparing pharmaceutically active ingredients.
参考标题:Synthesis Of N -Sulfonylformamidines By Tert -Butyl Hydroperoxide-Promoted, Metal-Free, Direct Oxidative Dehydrogenation Of Aliphatic Amines 作者:Ayijiamali Rouzi,Ruzeahong Hudabaierdi,Abudureheman Wusiman |发布日期:2018.5 摘要:A Direct And Convenient Metal-Free Method To Prepare Sulfonyl Amidines In The Presence Of Aqueous Tert-Butyl Hydroperoxide (T-Hydro) Has Been Developed. Different Tertiary And Secondary Amines Were Tested For Compatibility With The Oxidative Conditions And Could Be Coupled With Sulfonyl Azides To Form The Corresponding Amidines In Moderate To Good Yields.
合成参考文献
摘要:Scammells, P. J., Science of Synthesis Knowledge Updates, (2013) 2, 456. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).