CAS: 1051375-10-0; (3S,11Ar)-N-(2,4-Difluorobenzyl)-6-Hydroxy-3-Methyl-5,7-Dioxo-2,3,5,7,11,11A-Hexahydrooxazolo[3,2-A]Pyrido[1,2-D]Pyrazine-8-Carboxamide

上下游产品

(3R,11aS)-N-[(2,4-difluorophenyl)methyl]-3-methyl-5,7-dioxo-6-[(phenylmethyl)oxy]-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-2-carboxylate (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-3-methyl-5,7-dioxo-6-[(phenylmethyl)oxy]-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide methyl 2-[(dimethylamino)methylene]-4-methoxy-3-oxobutanoate{[(3S,11aR)-8-({[(2,4-difluorophenyl)methyl]amino}carbonyl)-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazin-6-yl]oxy}methyl methyl carbonate

麦芽醇置于吡啶,Sodium Periodate,N-溴代丁二酰亚胺(Nbs),四(三苯基膦)钯,Rhodium(III) Chloride Hydrate,Palladium 10% On Activated Carbon,水,氢气,碳酸氢钠,Potassium Carbonate,溶剂黄146,甲基磺酰氯,三乙胺,N,N-二异丙基乙胺,Lithium Hexamethyldisilazane体系中,用 四氢呋喃,N-甲基吡咯烷酮,甲醇,乙醇,水,二甲基亚砜,乙酸乙酯,乙腈 用作溶剂,化学反应 43.83H,反应生成(3S,11Ar)-N-[(2,4-二氟苯基)甲基]-2,3,5,7,11,11A-六氢-6-羟基-3-甲基-5,7-二氧代恶唑并[3,2-A]吡啶并[1,2-D]吡嗪-8-甲酰胺
参考文献:(3S,11Ar)-6-[(Phenylmethyl)Oxy]-3-Methyl-2,3,11,11A-Tetrahydrooxazolo[3,2-A]Pyrido[1,2-D]Pyrazine-5,7-Dione Of The Formula P-9 And/or (3S,11Ar)-6-[(Phenymethyl)Oxy]-8-Bromo-3-Methyl-2,3,11,11A-Tetrahydrooxazolo[3,2-A]Pyrido[1,2-D]Pyrazine-5,7-Dione Of The Formula P-10
标题:(3S,11Ar)-6-[(Phenylmethyl)Oxy]-3-Methyl-2,3,11,11A-Tetrahydrooxazolo[3,2-A]Pyrido[1,2-D]Pyrazine-5,7-Dione Of The Formula P-9 And/or (3S,11Ar)-6-[(Phenymethyl)Oxy]-8-Bromo-3-Methyl-2,3,11,11A-Tetrahydrooxazolo[3,2-A]Pyrido[1,2-D]Pyrazine-5,7-Dione Of The Formula P-10
摘要:这些化合物是制备治疗病毒感染,特别是hiv感染的治疗剂的中间体.这些化合物是p-9式和/或p-10式的(3S,11Ar)-6-[(苯甲基)氧基]-3-甲基-2,3,11,11A-四氢噁唑并[3,2-A]吡啶并[1,2-D]吡嗪-5,7-二酮和(3S,11Ar)-6-[(苯甲基)氧基]-8-溴-3-甲基-2,3,11,11A-四氢噁唑并[3,2-A]吡啶并[1,2-D]吡嗪-5,7-二酮.

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-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: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-8754214-B2
优先权日:2008-12-11
标题 :Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates

专利号:US-8624023-B2
优先权日:2008-12-11
标 题:Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates

专利号:EP-2376080-B1
优先权日:2008-12-11
标 题 :Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates