专利号:US-4384127-A 优先权日:1981-04-08 标 题:Process for synthesis of optically pure prostaglandin E2 and analogs thereof 发明人:FUCHS PHILLIP L 权利人:PURDUE RESEARCH FOUNDATION 摘要:The invention comprises a multi-step synthesis of l(-) prostaglandin E 2 . The special features of the synthesis include: (1) a triply-convergent conjugate-addition and alkylation reaction involving the 1,4-addition of a chiral vinyl lithium reagent to a chiral vinylsulfone to produce a sulfone-stabilized anion. This anion is alkylated in situ to produce the basic prostaglandin skeleton structure, which is then subjected to (2) an efficient peracid oxidation of a secondary amine to a β-silyloxy oxime; and (3) an alkali-catalyzed 1,4-elimination of an α-sulfonyl oxime to produce a vinyl nitroso intermediate. This intermediate is treated with borohydride to give a stereospecific 1,4-reduction which yields the bis-silyloxy oxime of l(-)PGE 2 . Hydrolysis of the oxime, with concurrent cleavage of the silyloxy protecting groups, affords l(-)PGE 2 .
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-4756739-A 优先权日:1985-12-21 标题 :Pyridine derivatives and the N-oxides thereof, and the use thereof as intermediates for the synthesis of plant protecting agents 发明人:FUSS ANDREAS; KOCH VOLKER 权利人:HOECHST AG 摘要:The compounds of the formula I (I) in which A denotes N or N->O, Z denotes O or NH, R denotes H, (halo)alkyl, (halo)alkenyl, (halo)alkynyl or alkoxycarbonyl, R1 denotes hydrogen, halogen, amino, -NHOH, hydroxyl, (substituted) phenylazo or a radical of the formulae Y=C=N-, Y1Y2C=N-, Y3NH- or K denotes 0 or 1, and m and n, independently of one another, denote a number from 1 to 4, with the proviso that, when Z-R denotes OH or NH2, (R1)n denotes at least one radical of the formula or represents two radicals, in the 5 or 6 position of the heterocyclic ring, which, in the 5 position, denote halogen and, in the 6 position, denote a radical of the group comprising halogen, amino, hydroxyl or phenylazo, which may be substituted as specified above, are valuable intermediates in the synthesis of plant protection agents.
专利号:US-9518034-B2 优先权日:2013-10-14 标题 :Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof 发明人:STOLTZ BRIAN M; DOUGHERTY DENNIS A; DUQUETTE DOUGLAS; DUFFY NOAH 权利人:CALIFORNIA INST OF TECHN 摘要:This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n ncomprising treating a compound of formula (II):n n nwith a transition metal catalyst under alkylation conditions.
专利号:US-12319712-B2 优先权日:2018-05-09 标 题:Methods of synthesizing a polynucleotide array using photoactivated agents 发明人:RAJASEKARAN JOHN J; JAYARAMAN VASANTH; VENUGOPAL ANIRUDH; BEI KANG; WANG TIANHAO; KRISHNA KARTHIK; KRISHNAMURTHY HARI KRISHNAN 权利人:VIBRANT HOLDINGS LLC 摘要:Described herein are methods for the synthesis of DNA polynucleotides and polynucleotides, as well as methods for their deprotection and methods for the use of said compounds and compositions comprising said compounds. In particular, such compounds and compositions comprising them are used in methods for light-directed synthesis of DNA microarrays.
专利号:US-2024261416-A1 优先权日:2023-01-31 标题:Synthesis of novel cereblon e3 ligase ligands, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; XIE HAIBO; WU YUNXIANG; LIAO JUNZHUO; LI CHUNRONG; TANDON IRA; TANG HUA 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.
摘要:Pearson, R. J., Science of Synthesis Knowledge Updates, (2012) 2, 230. 摘要:American Industrial Hygiene Association Journal., 40(600), 1979 [] 摘要:HITE M ET AL; ACUTE TOXICITY OF METHYL FLUOROSULFONATE (MAGIC METHYL); AM IND HYG ASSOC J 40(7) 600 (1979)