3446-89-7 = 874-87-3 反应条件:1.1 Reagents: Sodium Borohydride Solvents: Diethyl Ether; 2 - 3 H,10 - 15 °C; 15 °C -> Rt; 5 H,Rt2.1 Reagents: Hydrochloric Acid Solvents: Toluene,Water; 50 - 60 °C 标题:Preparation Of 4-(Methylthio) Phenylacetonitrile 作者:Hu,Xiao-Xue; Et Al 参考文献:Huaxue Shijie 日期:2010 卷标:51(10) 页码:626-628]
3446-90-0 + 98-88-4 = 874-87-3 反应条件:1.1 Catalysts: 1-Methoxy-2-(Methylsulfinyl)Benzene Solvents: Acetonitrile; 17 H,Rt 标题:Systematic Evaluation Of Sulfoxides As Catalysts In Nucleophilic Substitutions Of Alcohols 作者:Motsch,Sebastian; Et Al 参考文献:European Journal Of Organic Chemistry 日期:2018 卷标:2018(33) 页码:4541-4547]
3446-90-0 = 874-87-3 反应条件:1.1 Reagents: Thionyl Chloride Solvents: Dichloromethane; 0 °C; 2 H,Rt 标题:Solid-Phase Peptide Synthesis Using A Four-Dimensional (Safety-Catch) Protecting Group Scheme 作者:Noki,Sikabwe; Et Al 参考文献:Journal Of Organic Chemistry 日期:2022 卷标:87(15) 页码:9443-9453]
3446-90-0 = 874-87-3 反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Toluene,Water; 50 - 60 °C 标题:Preparation Of 4-(Methylthio) Phenylacetonitrile 作者:Hu,Xiao-Xue; Et Al 参考文献:Huaxue Shijie 日期:2010 卷标:51(10) 页码:626-628]
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-4536599-A 优先权日:1978-08-22 标题:Synthesis of amine derivatives 发明人:MASUKO FUJIO; KATSURA TADASHI 权利人:SUMITOMO CHEMICAL CO 摘要:An amine of the formula, ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are each hydrogen, alkyl or the like and n is 1, 2 or 3, including α-phenyl-β-(p-tolyl)-ethylamine, which is useful as an optically resolving agent, an intermediate of medicines and the like, is effectively produced by a novel process comprising hydrolysis of the corresponding nitrile of the formula, ##STR2## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above, followed by alkali-decomposition of the resulting amide of the formula, ##STR3## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above. An amide including the above one is effectively produced by hydrolysis of the corresponding nitrile in the presence of a base and hydrogen peroxide using an organic quaternary ammonium salt and/or a tertiary amine as a catalyst.
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:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related 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: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 权利人:LILLY CO ELI 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:US-11161823-B2 优先权日:2019-03-11 标 题 :Anticancer 1,3-dioxane-4,6-dione derivatives and method of combinatorial synthesis thereof 发明人:ISLAM IMADUL; AL-KAYSI RABIH O; BOUDJELAL MOHAMED; ALI RIZWAN; NEHDI ATEF; ALGHANEM BANDAR 权利人:NAT GUARD HEALTH AFFAIRS; KING SAUD BIN ABDULAZIZ UNIV FOR HEALTH SCIENCES; KING ABDULLAH INTERNATIONAL MEDICAL RES CENTER; KING ABDULLAH INETRNATIONAL MEDICAL RES CENTER 摘要:Compounds, methods of synthesis, and methods of cancer treatment by arylidene-1,3-dioxane-4,6-diones. A Meldrum's acid-based chemistry and hybrid solid-liquid method. The method includes protection of ketone and aldehyde components and simultaneous immobilization on the solid phase, introduction of substituents, grafts and derivatives compatible with the protection, detachment and restoration of active carbonyl reactivity, reaction of ketone library with malonate, reacting of the products with the aldehyde library in liquid phase and separation of the products by preparative HPLC.
专利号:US-3563958-A 优先权日:1968-04-02 标 题:Esterification of arylmethylene sulfonium resins with n - protected amino acids for use in solid-phase peptide synthesis 发明人:DORMAN LINNEAUS C 权利人:DOW CHEMICAL CO 摘要:THE MERRIFIELD SOLID-PHASE PEPTIDE SYNTHESIS IS IMPROVED BY BONDING THE AMINO ACID TO THE SUPPORTING RESIN THROUGH REACTION OF AN N-PROTECTED AMINO ACID (I) WITH AN ARYLMETHYLENE SULFONIUM RSIN (II) TO FORM AN AMINO ACID RESIN BENZYL ESTER (IV): P-NH-CH(-R)-COOH + X-AR-CH2-S(+)(-R1)-R2.Y(-) --> P-NH-CH(-R)-COO-CH2-AR-X ADVANTAGES OF THIS PROCESS INCLUDE BROADER SCOPE, MILD CONDITIONS, HIGHER RESIN ESTER CAPACITIES AND IMPROVED YIELDS. HIGHEST YIELDS ARE OBTAINED WHEN A BASIC SALT OF THE SULFONIUM RESIN IS USED.