CAS: 518048-05-0; N-(2-(4-((4-Fluorobenzyl)Carbamoyl)-5-Hydroxy-1-Methyl-6-Oxo-1,6-Dihydropyrimidin-2-yl)Propan-2-yl)-5-Methyl-1,3,4-Oxadiazole-2-Carboxamide

上下游产品

5-methyl-1,3,4-oxadiazole-2-carboxylic acid chloride 2-(1-amino-1-methyl-ethyl)-N-[(4-fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-6-oxo-4-pyrimidinecarboxamide 25H29FN6O6C25H29FN6O6 methyl 5-(benzoyloxy)-1-methyl-2-(1-methyl-1-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}ethyl)-6-oxo-1,6-dihydropyrimidine-4-carboxylateraltegravir diethylamine salt raltegravir diisopropylamine salt raltegravir tert-butylamine salt N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(1-methyl-1-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl] amino}ethyl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide sodium salt

4-((4-Fluorobenzyl)Carbamoyl)-1-Methyl-2-(2-(5-Methyl-1,3,4-Oxadiazole-2-Carboxamido)Propan-2-yl)-6-Oxo-1,6-Dihydropyrimidin-5-Yl 5-Methyl-1,3,4-Oxadiazole-2-Carboxylate 反应生成 雷特格韦
参考文献:寻求选择性和效率:Raltegravir合成的新方法
标题:寻求选择性和效率:Raltegravir合成的新方法
摘要:本工作描述了活性药物成分raltegravir的改良合成方法的发展.新工艺中间体的分离和新开发的条件解决了该生产工艺典型的选择性问题,而无需使用保护基,这使当前路线比以前报道的更加有效和可持续.与先前过程的效率比较证实了此处获得的结果.
DOI:10.1021/acs.Oprd.0C00155

专利信息

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-2016185745-A1
优先权日:2013-08-07
标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
发明人：SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
权利人:UNIV TEXAS
摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-11649285-B2
优先权日:2016-08-03
标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
发明人：KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
权利人:BIO TECHNE CORP
摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

专利号:US-9475799-B1
优先权日:2011-12-26
标 题 :Synthesis of Raltegravir
发明人：GURJAR MUKUND KESHAV; SONAWANE SWAPNIL PANDITRAO; MAIKAP GOLAKCHANDRA SUDARSHAN; PATIL GULABRAO DAGADU; SHINDE SHIVNATH BHAUPATIL; SHALIKRAO PANKAJ; MEHTA SAMIT SATISH
权利人:EMCURE PHARMACEUTICALS LTD
摘要:The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).

专利号:US-10370455-B2
优先权日:2014-12-05
标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists
发明人：MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL
权利人:IMMUNEXT INC
摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.