专利号:US-5623068-A 优先权日:1994-03-07 标 题:Synthesis of DNA using substituted phenylacetyl-protected nucleotides 发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; HANNA NAEEM B 权利人:BECKMAN INSTRUMENTS INC 摘要:Deoxyribonucleotide and ribonucleotide derivatives of the general formula I I wherein R1 represents -CR'R''-Ar, in which Ar is substituted aryl (as hereinafter defined) and R' and R'' are independently selected from the group consisting of hydrogen and lower alkyl; one of -R2 and R3 is a hydroxyl-protecting group and the other is a group suitable for synthesis of polynucleotides or for attachment of the nucleotide to a solid support; R4 is selected from the group consisting of hydrogen, -OH and protected hydroxyl; and B represents a divalent radical corresponding to a purine or pyrimidine base. When synthesis is carried out using these derivatives, the deprotection procedure is reduced to an essentially instantaneous process. The derivatives have acceptable shelf life and are very stable to conventional DNA synthesis conditions. Particularly preferred are those compounds wherein Ar is mono- and dihalo-substituted phenyl.
专利号:US-6951932-B2 优先权日:2001-10-25 标 题:Synthesis of 2-aralkoxyadenosines and 2-alkoxyadenosines 发明人:MOORMAN ALLAN R 权利人:KING PHARMACEUTICALS RES & DEV 摘要:The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.
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:US-7098354-B2 优先权日:2002-10-25 标 题:Racemoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indeyl)zirconium compounds 发明人:DAMRAU HANS-ROBERT; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a specific process for the diastereoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indenyl)zirconium compounds of the formula I, n nby reacting the silyl-bridged bisindenyl ligand with a dihalozirconium bis(3,5-di-tert-butylphenoxide)-base adduct to form the diorganosilylbis(2-methylbenzo[e]indenyl)zirconium bis(3,5-di-tert-butylphenoxide) and subsequently replacing the phenoxide groups by X using suitable replacement reagents to give the compound of the formula I; where the substituents X can be identical or different and are each F, Cl, Br, I or linear, cyclic or branched C 1-10 -alkyl; and the substituents R can be identical or different and are each linear, cyclic or branched C 1-10 -alkyl or C 6-10 -aryl; and also to the use of these compounds as catalysts.
专利号:US-3682895-A 优先权日:1970-07-17 标题 :Synthesis of 3-hydroxy-5-bufa-20,22-dienolide 发明人:PETTIT GEORGE R; FESSIER DYRAL C; PAUIL KENNETH D 权利人:GEORGE R PETTIT; DYRAL C FESSIER; KENNETH D PAUIL 摘要:THERE IS PROVIDED A NOVEL METHOD OF SYNTHEESIZING 5ABUFADIENOLIDES, WHICH ARE USEFUL INTERMEDIATES IN THE TOTAL SYNTHESIS OF BUFALIN, A CARDIAC ACTIVE COMPOUND. EPIANDROSTERONE ACETATE IS CONVERTED INTO 3B - ACETOXYL-5APREGNANE-21-AL WHICH UNDERGOES CHAIN EXTENSION TO METHYL 3B-ACETOXYL-20-FORMYL-21-NOR-5A-CHOLANATE WHICH IS RING CLOSED TO FORM THE 3B - ACETOXY-5-A-BUF-20(21)-ENOLIDE WHICH IS DEHYDROGENATED TO THE CORRESPONDING BUFADIENOLIDE.
专利号:US-5488131-A 优先权日:1994-03-23 标题:Synthesis of compounds with predetermined chirality 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A method for synthesizing enantiomerically enriched chemical intermediates with predetermined chirality is described. The method comprises formation of a pseudoephedrine amide, followed by stereoselective alkylation at the alpha carbon. The chiral auxiliary can then be cleaved off, affording chiral end products useful for further transformations. The enantiomeric enrichment of the chiral end products may exceed 98%, and the chiral auxiliary can be recovered. Novel amides of pseudoephedrine used in this method are also disclosed.
摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 128. 摘要:Nieto, C. T.; Eames, J.; Garrido, N. M., Science of Synthesis Knowledge Updates, (2019) 1, 101. 摘要:Bubnov, Yu. N.; Kolomnikova, G. D., Science of Synthesis Knowledge Updates, (2012) 3, 272. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 214. 摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 77.