专利号:US-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
专利号:US-3898264-A 优先权日:1970-08-26 标题:Steroid total synthesis process utilizing a cyanoalkyl A-ring precursor 发明人:COHEN NOAL; ROSENBERGER MICHAEL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents gamma -butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an Aring precursor without resorting to protective groups as was heretofore found necessary in previous steroid total synthesis processes.
专利号:US-2025073250-A1 优先权日:2022-01-05 标题:Improved synthesis of lysine acetylsalicylate - Glycine particles 发明人:NOCKER KARLHEINZ; ZUHSE RALF; VON SCHRADER THOMAS; BRAUNE CHRISTIAN 权利人:ASPIAIR GMBH 摘要:The invention provides an improved method for preparing lysine acetylsalicylateâ‹…glycine (LASAG) that allows for high yields without the need for an addition of seed crystal, as well as yielding controlled, small particle sizes (median particles size preferably <40 μm) and high stability of the LASAG. Advantageously, the method can be performed at room temperature without negatively impacting yield or particle properties. The invention also provides the LASAG obtained from said method, and its uses as a medicine.
专利号:US-3607338-A 优先权日:1968-04-11 标 题 :Synthesis of zinc titanate pigment and coatings containing the same 发明人:GATES DANIEL W; ZERLAUT GENE A; ROGERS FREDERICK O 权利人:NASA 摘要:Zinc titanate pigment resistant to degradation of reflective properties upon exposure to ultraviolet radiation in vacuum is prepared by reacting zinc oxide with anatase titanium dioxide at a molar ratio of 2:1 and a temperature of at least 900* C. and contacting the product with a zinc oxide extractant solution. The pigment prepared by this process is combined with a suitable binder to produce degradation-resistant coatings.
专利号:US-7390801-B2 优先权日:1996-12-23 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:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J 权利人:ATHENA NEUROSCIENCES INC; 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 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.