专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-11661406-B2 优先权日:2018-08-13 标 题 :Method for producing intermediate useful for synthesis of SGLT inhibitor 发明人:LI QING RI; YOON HEE KYOON 权利人:DAEWOONG PHARMACEUTICAL CO LTD 摘要:A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.
专利号:US-5936080-A 优先权日:1996-05-24 标题 :Compositions and methods for the synthesis of organophosphorus derivatives 发明人:STEC WOJCIECH J; WOZNIAK LUCYNA 权利人:GENTA INC; POLSKA AKADEMIA NAUK INSTYTUT 摘要:New organophosphorus mononucleoside derivatives, methods of their synthesis and methods for the synthesis of organophosphorus dinucleotide derivatives utilizing the organophosphorus mononucleosides are provided. Synthesized organophosphorus mononucleoside derivatives of the present invention are characterized by the formula; ##STR1## Organophosphorus dinucleoside derivatives prepared from the synthesis methods provided in the present invention are characterized by the formula; ##STR2##
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
参考标题:Development Of A Scalable Synthesis Of The Small Molecule Tgfβr1 Inhibitor Bms-986260 作者:Muthalagu Vetrichelvan,Souvik Rakshit,Sathishkumar Chandrasekaran,Karthikeyan Chinnakalai,Chetan Padmakar Darne,Dyamanna Doddalingappa,Indasi Gopikumar,Anuradha Gupta,Arun Kumar Gupta,Ananta Karmakar,Thirumalai Lakshminarasimhan,David K. Leahy,Senthil Palani,Vignesh Radhakrishnan,Richard Rampulla,Antony Savarimuthu,Varadharajan Subramanian,Upender Velaparthi,Jayakumar Warrier,Martin D. Eastgate,Robert M. Borzilleri,Arvind Mathur,Rajappa Vaidyanathan |发布日期:2020.7.17 摘要:(1) Was Developed. This Alternative Approach Circumvented The Purification Of Intermediates By Column Chromatography And Provided Access To Multikilogram Quantities Of The Key Intermediate, 6. The Safety Aspects Of The Synthetic Approach To The Other Fragment Of The Api (Tosmic 10) Were Critically Evaluated, And A Robust Process For Its Large-Scale Synthesis Was Successfully Demonstrated.