专利号:US-6482950-B1 优先权日:1991-05-06 标 题 :Squarylium compounds, and processes and intermediates for the synthesis of these compounds 发明人:GARCIA PAULINA P; LEE JOHN W; MARSHALL JOHN L; MCGOWAN DONALD A; PUTTICK ANTHONY J; SPENCER THOMAS K; STROUD STEPHEN G; TELFER STEPHEN J; ZURAW MICHAEL J 权利人:POLAROID CORP 摘要:Squarylium compounds of the formula: n wherein Q 1 and Q 2 are each independently a pyrylium, thiopyrylium, selenopyrylium, benzpyrylium, benzthiopyrylium or benzselenopyrylium nucleus, and R 1 and R 2 are each independently an aliphatic or cycloaliphatic group, can be prepared by reacting a squaric acid derivative of the formula: n with a compound of the formula Q 2 CH 2 R 2 in the presence of a base. The derivatives of Formula II may be prepared by condensing a 2,3,4,4-tetrahalocyclobut-2-en-1-one with a compound of the formula Q 1 CH 2 R 1 in the presence of a base to produce a compound of the formula: n wherein Q 1 and R 1 are as defined above, and X represents chlorine or bromine, and hydrolyzing the compound of Formula III. Alternatively, the derivatives of Formula II may be prepared by reacting a diester, monoacid chloride monoester or diacid chloride of squaric acid with a compound of the formula Q 1 CH 2 R 1 in the presence of a base, followed by hydrolysis of the resultant monoacid chloride or monoester derivative of the compound of Formula II to the parent compound.
专利号:WO-0069864-A1 优先权日:1999-05-19 标 题 :An improved synthesis of tetrakis (dihydro carbylamino) phosphonium halides 发明人:FLETCHER MICHELLE O; DEVROU PHILIP R; BALHOFF JOHN F; ATKINSON BRIAN 权利人:ALBEMARLE CORP 摘要:An improved, commercially viable process for synthesizing tetrakis(dihydrocarbylamino)phosphonium halides in the absence of oxigen is described. When reacting a tris(dihydrocarbylamino)phosphinimine with a halohydrocarbon and an aqueous solution of a source of hydroxide ion to form a tetrakis(dihydrocarbylamino)phosphonium halide, a combination of increased pressure and liquid organic medium is used. The advantages gained by operating in this fashion include shorter reaction times and the need for only about stoichiometric or slightly more than stoichiometric amounts of halohydrocarbon and source of hydroxide ion.
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-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.
专利号:WO-9967219-A1 优先权日:1998-06-22 标 题:Compounds for inhibiting beta-amyloid peptide release and/or its synthesis 发明人:AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING 摘要:Compounds of formula (I), wherein W is a cyclic group of the type (2); (3); Y is represented by the formula (II); these compounds inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising 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.
专利号:WO-9966934-A1 优先权日:1998-06-22 标 题 :CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 发明人:AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 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 comprising 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.
[参考文献]: Usama M Hegazy, Et Al. Replacement Surgery With Unnatural Amino Acids In The Lock-And-Key Joint Of Glutathione Transferase Subunits. Chem Biol. 2006 Sep;13(9):929-36.
合成参考文献
参考文献:10.1134/s1070363216120367 摘要:Khalifa NM, Al-Omar MA, Amr AE. Synthesis and characterization of novel 5-allyl-6-{(benzo[d]thiazol-2-yl)methyl}-2-(alkylsulfanyl)oxopyrimidine derivatives. Russian Journal of General Chemistry. 2016 Dec;86(12):2752–8. doi: 10.1134/s1070363216120367.