专利号:US-7078572-B2 优先权日:2002-09-20 标题:Process for the synthesis of intermediates useful for the synthesis of tubulin inhibitors 发明人:KENDALL JOHN THOMAS 权利人:WYETH CORP 摘要:The invention is a process for the preparation of compounds of the Formula I: n nwhere R 1 , R 2 , R 3 , R 4 and R 5 are defined in the specification, which are intermediates useful for the preparation of tubulin inhibitors which are useful in the treatment of cancer.
专利号:US-7230135-B2 优先权日:2000-12-13 标 题 :Synthesis of P-chiral bisphospholane ligands and their transition metal complexes for use as asymmetric hydrogenation catalysts 发明人:HOGE II GARRETT STEWART; GOEL OM PRAKASH 权利人:WARNER LAMBERT CO 摘要:P-chiral bisphospholane ligands and methods for their preparation are described. Use of metal/P-chiral bisphospholane complexes to catalyze asymmetric transformation reactions to provide high enantiomeric excesses of formed compounds is also described.
专利号:US-6800764-B2 优先权日:2001-12-11 标题:Process for the synthesis of chirally pure beta-amino-alcohols 发明人:KREFT ANTHONY FRANK; ANTANE MADELENE MIYOKO; COLE DEREK CECIL; KUBRAK DENNIS MARTIN; RESNICK LYNN; STOCK JOSEPH RAYMOND; WANG ZHENG 权利人:WYETH CORP 摘要:A process is provided for preparing chirally pure S-enantiomers of alpha-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an alpha-azido acid; h) reducing the alpha-azido acid to the alpha-amino acid; and i) recrystallizing the alpha-amino acid to the chirally pure alpha-amino acid. A process is also provided for preparing chirally pure S-enantiomers of beta-amino alcohols further comprising the steps of reducing the crude alpha-amino acid to the beta-amino alcohol and recrystallizing the beta-amino alcohol to the chirally pure beta-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl beta-amino alcohols further comprising the steps of sulfonylating the beta-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl beta-amino alcohols.
专利号:US-6670477-B2 优先权日:2001-03-14 标题:Synthesis of enantiomerically enriched 4-piperidinylglycine 发明人:SHIEH WEN-CHUNG; XUE SONG; REEL NOELA MARJORY; FITT JOHN JOSEPH 权利人:NOVARTIS AG 摘要:A process for making enantiomerically enriched 4-piperidinylglycine having the formula (I),said process comprising (a) combining N-protected glycine ester with 4-piperidone to form didehydroamino acid ester; (b) reducing the didehydroamino acid ester with hydrogen gas in the presence of a rhodium catalyst selected from the group consisting of (R,R)-BPE-Rh; (S,S)-BPE-Rh; (R,R)-DuPHOS-Rh; (S,S)-DuPHOS-Rh; and combinations thereof; whereby a protected compound is formed; and (c) removing the protecting groups from the protected compound, whereby the 4-piperidinylglyeine having the formula (I) is formed, wherein X<- >is an anion wherein X is independently a halogen; and '*' designates an asymmetric carbon having (R)- or (S)-configuration. The process of the invention yields an enantiomerically enriched (R)-4-piperidineglycine or (S)-4-piperidineglycine.
专利号:US-5994559-A 优先权日:1998-08-06 标题:Synthesis of monatin-A high intensity natural sweetener 发明人:ABUSHANAB ELIE; ARUMUGAM SUBRAMANIAM 权利人:RHODE ISLAND EDUCATION 摘要:The high intensity natural sweetener monatin, an α-amino acid (1) is synthesized from readily available starting materials. Regiospecific ring opening of epoxide (9) with indole magnesium bromide yields lactone (11). Amination of (11) followed by saponification yields Monatin.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 223. 摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 79. 摘要:Driver, T. G., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 322. 摘要:Mace Weldy, N.; Blakey, S. B., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 264. 摘要:Cahoon, S. B.; Yoon, T. P., Science of Synthesis, (2021) , 181.