环戊基氨基甲酸叔丁酯置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 用作溶剂,化学反应 40.0H,反应生成环戊基甲基胺 参考文献:7-Azaindole Or 4,7-Diazaindole Derivatives As Ikk Epsilon And Tbk1 Inhibitor And Pharmaceutical Composition Comprising Same 标题:7-Azaindole Or 4,7-Diazaindole Derivatives As Ikk Epsilon And Tbk1 Inhibitor And Pharmaceutical Composition Comprising Same 摘要:提供了7-氮杂吲哚或4,7-二氮杂吲哚衍生物作为ikkε(i-卡帕b激酶ε)和tbk1(tank结合激酶1)抑制剂.7-氮杂吲哚或4,7-二氮杂吲哚衍生物有效地抑制ikkε和tbk1,因此不仅可用作抗癌剂治疗各种癌症,包括结直肠癌,乳腺癌,中枢神经系统癌,结肠癌,非小细胞肺癌,肾癌,前列腺癌,卵巢癌,子宫癌,胃癌,肝癌,皮肤癌,肺癌,脑癌,膀胱癌,食管癌,胰腺癌,甲状腺癌,头颈癌,鳞状细胞癌,骨肉瘤,B细胞或t细胞淋巴瘤,急性或慢性白血病和多发性骨髓瘤,还可作为慢性炎症的治疗剂.
专利号:US-9005573-B2 优先权日:2011-12-22 标 题:Layered conversion synthesis of zeolites 发明人:NICHOLAS CHRISTOPHER P; MILLER MARK A 权利人:UOP LLC 摘要:A new synthesis technique has been developed to prepare a family of coherently grown composites of at least two zeotypes. Examples of these composites are represented by the empirical formula.n nNa n M m k+ T t Al 1-x E x Si y O z n nwhere “nâ€? is the mole ratio of Na to (Al+E), M represents at least one metal of zinc, Group 1, Group 2, Group 3 and the lanthanide series of the periodic table, and any combination thereof, “mâ€? is the mole ratio of M to (Al+E), “kâ€? is the average charge of the metal or metals M, T is the organic structure directing agent or agents, “tâ€? is the mole ratio of N from the organic structure directing agent or agents to (Al+E), and E is a framework element such as gallium. The synthesis technique is the Layered Conversion Synthesis technique.
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:US-9458111-B2 优先权日:2010-07-29 标题:Process for the synthesis of substituted urea compounds 发明人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS 权利人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS; BIAL—PORTELA & CA S A 摘要:A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof: n nthe process comprising the reaction of a carbamate of Formula (II′): Formula (I′):n n nwith a primary or secondary amine of the formula R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
专利号:WO-2011148392-A1 优先权日:2010-05-28 标题 :Process for the preparation of (2s,4s,5s,7s)-n-(2-carbamyl-2- methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3- methoxypropoxy)phenyl]-octanamide hemifumarate and its intermediates thereof 发明人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY 权利人:MSN LAB LTD; SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY 摘要:The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.
专利号:US-11078163-B2 优先权日:2014-01-24 标 题 :Processes for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & CA SA; BIAL PORTELA & Cª S A 摘要:The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, the process comprising the reaction of an imidazolyl intermediate of Formula IIa′ with a carbamoyl halide of the formula: R1R2NC(â•?O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa′ is prepared by oxidation of the derivative of R5 and R6, R6-C(â•?O)CH2R5 to form a glyoxal intermediate R6-C(â•?O)(Câ•?O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa′ and wherein the compound substituents are as defined herein.
专利号:US-5245069-A 优先权日:1992-10-27 标题:Process for the preparation of bis(aryl)-phosphorohalidates 发明人:MCMANUS JAMES W 权利人:MERCK & CO INC 摘要:This invention relates to a novel process for preparing bis(aryl)phosphorohalidates which are useful in the synthesis of various enol phosphates. The process of this invention provides a means of producing a high-yield, high-purity product without the need for costly crystallization or impractical, high temperature distillations.
摘要:M. Mousseron and P. Froger. Bull. Soc. Chim. France 1947, 843. 摘要:Zaidlewicz, M.; Krzeminski, M., Science of Synthesis, (2005) 6, 1148. 摘要:Lawrence, S. A., Science of Synthesis, (2009) 40, 539.