专利号:WO-2024181781-A1 优先权日:2023-02-27 标 题:Substrate for synthesis of biological polymers having anti-aggregation function and biological polymer synthesis method using same 发明人:JANG MYOUNG HOON; CHOI JAE SUN 权利人:SP2 TX INC 摘要:The present invention relates to a substrate for the synthesis of biological polymers having an anti-aggregation function, and a biological polymer synthesis method using the substrate. The substrate according to an aspect may have anti-aggregation functionality to enable high-yield and high-purity processes in the synthesis of biological polymers.
专利号:US-6531591-B1 优先权日:1999-07-07 标 题 :Synthesis of stable quinone and photoreactive ketone phosphoramidite reagents for solid phase synthesis of photoreactive-oligomer conjugates 发明人:FENSHOLDT JEF 权利人:EXIQON AS 摘要:Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.
专利号:US-7612210-B2 优先权日:2005-12-05 标题:Process for selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols 发明人:MAHANEY PAIGE ERIN; ANTANE MADELENE MIYOKO; SUN JERRY SHUNNENG 权利人:WYETH CORP 摘要:A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4-benzyloxazolidinone with a mixed anhydride of a methyoxyphenylacetic acid under conditions which form a oxazolidinone, (4S)- or (4R)-4-benzyl-3-[methyoxyphenyl]acetyl]-oxazolidin-2-one, (b) treating the (4S)- or (4R)-4-benzyl-3-[(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one with an aprotic amine base and titanium chloride in a chlorinated solvent under conditions which permit formation of the corresponding anion, (c) mixing the corresponding anion with titanium chloride and cylcohexanone under conditions which permit an aldol reaction to form the corresponding (4S)- or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one,(d) hydrolyzing the (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one to form a chiral acid (2S or 2R)-(1-hydroxycyclohexyl)-methoxyphenyl)acetic acid, (e) coupling the chiral phenylacid to a secondary amine to form an amide, and (f) reducing the amide to form an (S) or (R) 1[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol or a salt thereof.
专利号:US-4704450-A 优先权日:1983-02-21 标 题 :Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate peptides 发明人:DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY 权利人:SANOFI SA 摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
专利号:US-12435086-B2 优先权日:2020-04-29 标题:Synthesis of heterocyclic compounds 发明人:LIN JACK; WALTERS JASON 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of Formula 2:wherein R1 is C(O)R2; R2 is alkyl optionally substituted with 1-5 halogens; G is phenyl or a 5-6 membered heteroaryl optionally substituted with 1-2 R3; and each R3 is independently C1-C6 alkyl, CN, C1-C6 alkyl-CN, 3-6 membered cycloalkyl, or 4-6 membered heterocycloalkyl.
专利号:US-11708341-B2 优先权日:2016-08-05 标题:Synthesis of (S)-2-amino-4-methyl-((R)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof 发明人:Beaver Matthew; CUI SHENG; SHI XIANGQING 权利人:AMGEN INC 摘要:The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure n nCompound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.
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合成参考文献
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