专利号:US-11708363-B2 优先权日:2020-09-30 标 题:Method for preparing a key intermediate for the synthesis of statins 发明人:CHEN FENER; CHENG DANG; LIU MINJIE; HUANG ZEDU; TAO YUAN; WANG JIAQI 权利人:UNIV FUDAN 摘要:Disclosed herein relates to organic synthesis, and more particularly to a method for preparing a key intermediate for the synthesis of statins. The key intermediate is 2-[(4R,6S)-6-[(benzo[d]thiazol-2-ylthio)methyl]-2,2-disubstituted-1,3-dioxan-4-yl] acetate of formula (I): n nwhere R 1 is a C 1 -C 8 alkyl group, a C 3 -C 8 cycloalkyl group, a monosubstituted or polysubstituted aryl group, or monosubstituted or polysubstituted aralkyl group; R 2 is hydrogen, or monosubstituted or polysubstituted C 1 -C 3 alkyl group, or halogen; and R 3 and R 4 are each independently a C 1 -C 5 alkyl group, a C 3 -C 7 cycloalkyl group, a C 3 -C 7 cycloalkenyl group, a C 1 -C 3 alkoxy group, a C 6 -C 10 aryl group, or C 7 -C 12 aralkyl group. In the method, a halomethyl compound and a thiol reagent are subjected to nucleophilic substitution in an organic solvent to synthesize a thioether, which then undergoes ketal exchange reaction with a carbonyl compound (V) in the presence of an organic acid to obtain a target product.
专利号:US-5919969-A 优先权日:1996-06-05 标 题 :Synthesis of yellow couplers 发明人:CRAWLEY MICHAEL W 权利人:EASTMAN KODAK CO 摘要:The invention provides a method of synthesis of a image-dye forming coupler of formula (I) wherein X is a substituent linked to the coupler by an atom of oxygen, sulfur or nitrogen R1 is an alkyl or aryl group, R2 is a hydrogen atom or an alkyl group; R3 to R7 are the same or different and selected from a hydrogen atom and substituent groups; which method comprises the reaction of a compound of formula (II) wherein R and R1 are the same or different and are as defined above for R1 and X is as defined above with a compound of formula (III) wherein R2 to R7 are as defined above, in the presence of an inert organic solvent.
专利号:US-6159673-A 优先权日:1996-07-17 标 题:Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
专利号:US-9409945-B2 优先权日:1999-10-04 标 题 :Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery 发明人:DESLONGCHAMPS PIERRE; DORY YVES; BERTHIAUME GILLES; OUELLET LUC; LAN RUOXI 权利人:OCERA THERAPEUTICS INC 摘要:A library of macrocyclic compounds of the formula (I) n n n n n n n n n n n n where part (A) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; n where part (B) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; n where part (C) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) t — bivalent radical, or a covalent bond; and n where part (T) is a —Y-L-Z— radical wherein Y is CH 2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:EP-1473330-B1 优先权日:1996-07-17 标题:Process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which each of Z, W<1> and W<2> independently is an atomic group that forms a heterocyclic ring; and M is a cation. A process for the synthesis of an oxonol compound is disclosed.
1: Jing P, Hou M, Zhao P, Tang X, Wan H. Adsorption of 2-mercaptobenzothiazole from aqueous solution by organo-bentonite. J Environ Sci (China). 2013 Jun 1;25(6):1139-44. doi: 10.1007/s11356-014-3131-1. Epub 2014 Jun 11. doi: 10.1016/j.saa.2015.06.108. Epub 2015 Jun 29. doi: 10.1007/s00103-015-2212-8. German. doi: 10.1039/c4cp03867c. doi: 10.1007/s00216-015-8533-5. Epub 2015 Feb 21. doi: 10.1021/ic5013236. Epub 2014 Sep 10. doi: 10.1007/s00216-015-8673-7. Epub 2015 Apr 23. doi: 10.1016/j.jes.2016.01.019. Epub 2016 Mar 10. doi: 10.1016/j.ejmech.2014.02.017. Epub 2014 Feb 11. doi: 10.1021/acs.est.5b04716. Epub 2016 Jan 8. doi: 10.1016/j.jes.2014.05.029. Epub 2014 Oct 22. doi: 10.1016/j.aca.2014.01.042. Epub 2014 Jan 30. doi: 10.1038/srep26044. 17: Xanthopoulou MN, Hadjikakou SK, Hadjiliadis N, Schürmann M, Jurkschat K, Michaelides A, Skoulika S, Bakas T, Binolis J, Karkabounas S, Charalabopoulos K. Synthesis, structural characterization and in vitro cytotoxicity of organotin(IV) derivatives of heterocyclic thioamides, 2-mercaptobenzothiazole, 5-chloro-2-mercaptobenzothiazole, 3-methyl-2-mercaptobenzothiazole and 2-mercaptonicotinic acid. J Inorg Biochem. 2003 Aug 1;96(2-3):425-34. doi: 10.1097/DER.0b013e3182a8c1ab. doi: 10.1016/j.aquatox.2012.10.013. Epub 2012 Oct 29. doi: 10.3797/scipharm.1204-27. Epub 2012 Jun 18.
合成参考文献
参考文献:10.1007/s00128-011-0360-6 摘要:Yi X, Kim E, Jo H, Han T, Jung J. A Comparative Study on Toxicity Identification of Industrial Effluents Using Daphnia magna. Bulletin of Environmental Contamination and Toxicology. 2011 Jul 15;87(3):319. doi: 10.1007/s00128-011-0360-6. 参考文献:10.1155/2011/982410 摘要:van Philips LAM. Toxic Anterior Segment Syndrome after Foldable Artiflex Iris-Fixated Phakic Intraocular Lens Implantation. Journal of Ophthalmology. 2011;2011():1–5. doi: 10.1155/2011/982410. 参考文献:10.1007/s00253-011-3471-4 摘要:Ghosh JS, Rokade KB. Biodegradation of 2-mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate by Pseudomonas desmolyticum NCIM 2112. Applied Microbiology and Biotechnology. 2011 Jul 20;93(2):753–61. doi: 10.1007/s00253-011-3471-4.