CAS: 1051375-16-6; (4R,12As)-N-(2,4-Difluorobenzyl)-7-Hydroxy-4-Methyl-6,8-Dioxo-3,4,6,8,12,12A-Hexahydro-2H-Pyrido[1',2':4,5]Pyrazino[2,1-B][1,3]Oxazine-9-Carboxamide

上下游产品

(4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2':4,5]-pyrazino[2,1-b][1,3]oxazine-9-carboxamide 15H20ClNO7C15H20ClNO7 13H14ClNO6C13H14ClNO6 15H17ClN2O5C15H17ClN2O5(4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2′:4,5]pyrazino-[2,1-b][1,3]oxazine-9-carboxamide sodium salt

Diethyl(Ethoxymethylene)Oxalacetate置于吡啶,Magnesium Bromide Ethyl Etherate,N,N'-羰基二咪唑,Sodium Hydroxide体系中,用 二氯甲烷 用作溶剂,化学反应 121.0H,反应生成度鲁特韦
参考文献:人类免疫缺陷病毒整合酶抑制剂多替拉韦钠的六步革兰氏规模合成
标题:人类免疫缺陷病毒整合酶抑制剂多替拉韦钠的六步革兰氏规模合成
摘要:开发了一种用于制备活性药物成分多替拉韦钠的简短实用的合成方法.收敛策略从 ( R )-3-氨基-1-丁醇开始,并在四个步骤中以 76% 的分离产率建立了 Bc 环系统.通过一锅1,4-加成到二乙基-( 2E / Z )-2-(乙氧基亚甲基)-3-氧代丁二酸和随后的mgbr 2 .oet 2介导的区域选择性环化来构建环a.与 2,4-二氟苄胺形成酰胺是通过游离羧酸或通过相应乙酯的氨解进行的.最终的盐形成通过六个线性步骤以 48-51% 的分离产率(HPLC 纯度为 99.7-99.9%)提供了多替拉韦钠.
Doi:10.1021/acs.Oprd.1C00139

专利信息

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-2025034607-A1
优先权日:2021-12-03
标题 :Process of Synthesizing (R)-3-aminobutan-1-ol
发明人：BOBKO MARK; FUERST DOUGLAS; MORGAN CHRISTOPHER
权利人:VIIV HEALTHCARE CO
摘要:The present invention relates to an aminotransaminase useful in the synthesis of (R)-3-aminobutan-1-ol (RABO). The present invention also provides a process of preparing (R)-3-aminobutan-1-ol (RABO) with the disclosed aminotransaminase.

专利号:US-9365587-B2
优先权日:2008-12-11
标 题:Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
发明人：YOSHIDA HIROSHI; TAODA YOSHIYUKI; JOHNS BRIAN ALVIN; KAWASUJI TAKASHI; NAGAMATSU DAIKI
权利人:SHIONOGI & CO; VIIV HEALTHCARE CO
摘要:The invention is a process for the preparation of a compound of the following formula (I): n nwherein R is —CHO, —CH(OH) 2 or —CH(OH)(OR 4 ); P 1 is H or a hydroxyl protecting group; P 3 is H or a carboxy protecting group; R 3 is H, halogen, hydroxy, optionally substituted lower alkyl, optionally substituted cycloalkyl, etc.; R x is H, halogen or R 2 —X—NR 1 —C(O)—; etc. as defined in the specification. The compounds are useful as intermediates in synthesizing compounds having HIV integrase inhibitory activity.

专利号:WO-2015019310-A1
优先权日:2013-08-07
标 题 :Process for the preparation of dolute-gravir and intermediates thereof
发明人：DANDALA RAMESH; VELLANKI SIVA RAM PRASAD; NADELLA MADHU MURTHY; BALUSU PHANI KUMAR
权利人:MYLAN LAB LTD
摘要:The present disclosure relates to processes for the preparation of dolutegravir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of dolutegravir.

专利号:US-11248005-B2
优先权日:2019-07-08
标 题 :Process for preparation of intermediates used for the synthesis of HIV integrase inhibitor
发明人：JADHAV HARISHCHANDRA SAMBHAJI; SHRIVASTAVA DHANANJAI; AHER UMESH PARASHARAM; DEOKAR SHARAD CHANDRABHAN; NALE DEEPAK BABASAHEB; HONRAO SURYAKANT TUKARAM; SINGH GIRIJ PAL
权利人:LUPIN LTD
摘要:Provided herein is a process for the intermediates used for preparation of HIV Integrase Inhibitor such as Bictegravir, Dolutegravir, Cabotegravir or their pharmaceutically acceptable salts.

专利号:US-2024207302-A1
优先权日:2021-04-01
标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof
发明人：CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.