专利号:US-2006199958-A1 优先权日:2003-04-14 标 题 :Process and intermediates for the preparation of pyrrolidine carboxylic acids 发明人:CVETOVICH RAYMOND; CHUNG JOHN Y; AMATO JOSEPH S; DIMICHELE LISA 权利人:CVETOVICH RAYMOND; CHUNG JOHN Y; AMATO JOSEPH S; DIMICHELE LISA 摘要:A novel process is provided for the preparation of pyrrolidine carboxylic acids, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, sexual dysfunction, male sexual dysfunction, and female sexual dysfunction.
专利号:US-6191277-B1 优先权日:1998-04-29 标 题:Hydroxypropylamide peptidomimetics as inhibitors of aspartyl proteases 发明人:DOLLE III ROLAND ELLWOOD; CAVALLARO CULLEN LEE; HERPIN TIMOTHEE FELIX 权利人:PHARMACOPEIA INC 摘要:Compounds of Formula Iare disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.
专利号:US-5144074-A 优先权日:1988-02-24 标 题:Process for the synthesis of carboxamides 发明人:LISTEMANN MARK L; PIERANTOZZI RONALD; ARMOR JOHN N 权利人:AIR PROD & CHEM 摘要:Carboxamides having the structural formula: n n R.sup.1 CHR.sup.2 CH(OR.sup.3)NHCR.sup.4 O n n wherein: n R 1 is H, C 1 -C 6 alkyl or aryl; n R 2 is H, C 1 -C 6 alkyl; n R 3 is benzyl, C 1 -C 8 alkyl or hydroxyalkyl; and n R 4 is H, C 1 -C 6 alkyl or aryl; n are synthesized by reacting an aldehyde having the structural formula: R 1 CHR 2 CHO wherein R 1 and R 2 are as defined above, with an alcohol having the structural formula: R 3 OH, wherein R 3 is as defined above, and an amide having the structural formula: R 4 CONH 2 wherein R 4 is as defined above, in the presence of a strong acid catalyst at a temperature in the range of 0°-200° C.
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-10772971-B2 优先权日:2017-06-22 标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates 发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V 权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC 摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.
专利号:US-5635598-A 优先权日:1993-06-21 标 题:Selectively cleavabe linners based on iminodiacetic acid esters for solid phase peptide synthesis 发明人:LEBL MICHAL; KRCHNAK VIKTOR; KOCIS PETR; LAM KIT S 权利人:SELECTIDE CORP 摘要:The present invention is directed to linkers based on ester bond linkages, especially iminodiacetic acid ester bond linkages, for use in solid phase peptide synthesis. In particular, the invention is directed to cleavable linkers that can release peptide from the solid phase support under relatively mild conditions by formation of a diketopiperazine or other cyclic structure, such that the cyclic structure remains on the solid phase support, and, in a second cleavage, under more stringent conditions of high pH. The invention is further directed to solid phase supports prepared with multiple cleavable linkers, including a linker that is cleaved by formation of a cyclic product. One such second linker is an ester of hydroxymethylbenzoic acid, or esters formed by carboxy groups of aspartic or glutamic acid.
参考文献:10.1021/jf0495486 摘要:Stadler RH, Robert F, Riediker S, Varga N, Davidek T, Devaud S, Goldmann T, Hau J, Blank I. In-depth mechanistic study on the formation of acrylamide and other vinylogous compounds by the maillard reaction. J Agric Food Chem. 2004 Aug 25;52(17):5550–8. doi: 10.1021/jf0495486.