专利号:US-5852198-A 优先权日:1996-04-03 标题 :Wittig reagents and method for preparing α,β-unsaturated phosphonates 发明人:XU YIBO; FLAVIN MICHAEL T; XU ZE-QI 权利人:MEDICHEM RES INC 摘要:Wittig-type reagents and methods of preparation and use thereof for preparing alpha , beta -unsaturated phosphonate esters from aldehydes and ketones are disclosed. The Wittig-type reagents have the following formulae: I II wherein X represents triflate, halide, BF4, SbF6, or ClO4; R1 represents alkyl, aryl or arylalkyl; and R2 represents alkyl, aryl or arylalkyl, provided that R1 and R2 not represent phenyl at the same time. The Wittig reagent diethyl phosphono-methylidenetriphenylphosphorane (1b) has been successfully synthesized for the first time via its phosphonium triflate salt (4a), by treating diethyl phosphonomethyltriflate with triphenylphosphine according to the disclosed method. The procedure has been applied to the synthesis of other new Wittig-type reagents such as phosphoranes and phosphonium salts. The new Wittig reagents thus synthesized were treated with various aldehydes and an activated ketone, affording the corresponding alpha , beta -unsaturated phosphonates, saturated phosphonates or phosphoric acids. Triphenylphosphorane 1b and triphenylphosphonium 4a led to both cis and trans isomers with the latter being predominant, while trans isomers were almost exclusively formed when tributyl reagents (1c and 4d) were used.
专利号:US-9096624-B2 优先权日:2009-06-01 标 题:Amino pyrimidine anticancer compounds 发明人:CREW ANDREW P; SHERMAN DAN; APPARI RAMA DEVI; CHEN XIN; CHILUKURI RAMESH; DONG HANQING; FERRARO CATERINA; FOREMAN KENNETH; GUPTA RAMESH C; LI AN-HU; STOLZ KATHRYN M; VOLK BRIAN; ZAHLER ROBERT 权利人:OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula 1, as shown below and defined herein: n n n n n n n n n n n n and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
摘要:Coote, S. C.; Smith, L. H. S.; Procter, D. J., Science of Synthesis Knowledge Updates, (2010) 3, 436. 摘要:Ielo, L.; Pace, V., Science of Synthesis: Knowledge Updates, (2025) 2. 参考文献:10.1021/ol026281s 摘要:Cheng F, Murata Y, Komatsu K. Synthesis, X-ray Structure, and Properties of the Singly Bonded C60 Dimer Having Diethoxyphosphorylmethyl Groups Utilizing the Chemistry of C602-. Org. Lett. 2002 Jun 21;4(15):2541–4. doi: 10.1021/ol026281s.