在 盐酸体系中,用78%的收率获得苄脒盐酸盐 参考文献:的制备n,N,N-'-三(三甲基硅烷基)脒; 取代未取代am的简便方法 标题:的制备n,N,N-'-三(三甲基硅烷基)脒; 取代未取代am的简便方法 摘要:三(三甲基甲硅烷基)am Rc(nsime 3)n(sime 3)2(r C 6 H 5,P-Ch 3 C 6-H 4,P-Clc 6 H 4,P-Meoc 6 H 4,P-Me 2 Nc 6 H 4,P-Cf 3 C 6 H 4,P-C 6 H 5 C 6 H 4通过使各自的腈与(me 3 Si)2 Nli.oet 2在醚中反应,得到中间体rc(nli)n(sime 3)2,制备cf 3和cf 3).将这些中间体与在甲苯中的clsime 3一起加热,以高收率得到产物,通过真空蒸馏将其分离.对于1,4-二氰基苯,两当量的试剂提供了全(三甲基甲硅烷基)-1,4-二m.用6 N乙醇hcl水解中间体,得到未取代的am盐酸盐rc(nh)nh 2 .hcl(rc 6-H 5,P-Meoch 6 H4,对-Clc 6 H 4,对-O 2 Nc 6 H 4)高收率. Doi:10.1016/0022-328X(87)80017-7
专利号:US-5856356-A 优先权日:1996-06-17 标题:Use of strontium salts and pharmaceutical compositions thereof for the treatment of arthrosis 发明人:TSOUDEROS YANNIS; DELOFFRE PASCALE; WIERZBICKI MICHEL 权利人:ADIR 摘要:The invention relates to the use of strontium salts and pharmaceutical compositions thereof for the treatment of arthrosis through stimulation of the synthesis of proteoglycans and type II collagen by chondrocytes.
专利号:WO-9815532-A1 优先权日:1996-10-09 标 题:Solid phase synthesis of heterocyclic compounds 发明人:MARZINZIK ANDREAS; FELDER EDUARD 权利人:CIBA GEIGY AG; MARZINZIK ANDREAS; FELDER EDUARD 摘要:Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept. The reaction sequence comprises the following steps: a) a solid carrier having reactive surface groups is loaded directly or via a spacer group with a compound bearing an aldehyde or a methylketon function, b) said function is modified using the Witting reaction or the aldol condensation, c) the heterocyclic ring is closed using a compound comprising two nucleophiles, wherein at least one of the said nucleophiles is NH2.
专利号:US-5688763-A 优先权日:1987-06-12 标题 :Compositions and methods for the synthesis of growth hormone receptor and growth hormone binding protein 发明人:HAMMONDS JR R GLENN; LEUNG DAVID W; SPENCER STEVEN A; WOOD WILLIAM I; COLOSI PETER CAMERON 摘要:Growth hormone receptor and growth hormone binding protein are purified enabling amino acid sequence and DNA isolates coding for growth hormone receptor and growth hormone binding protein and methods of obtaining such DNA are provided, together with expression systems for recombinant production of growth hormone receptor and growth hormone binding protein. Therapeutically useful forms of the growth hormone receptor and growth hormone binding protein and anti-receptor antibodies are described.
专利号:US-4713383-A 优先权日:1984-10-01 标 题:Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses 发明人:FRANCIS JOHN E; GELOTTE KARL O 权利人:CIBA GEIGY CORP 摘要:[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula wherein R1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R2 is hydrogen or lower alkyl; X is oxygen or NR3, R3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N-R3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N-R3.
专利号:US-5057417-A 优先权日:1987-06-12 标题 :Compositions and methods for the synthesis of growth hormone receptor and growth hormone binding protein 发明人:HAMMONDS R GLENN; LEUNG DAVID W; SPENCER STEVEN A; WOOD WILLIAM I 权利人:GENENTECH INC 摘要:Growth hormone receptor and growth hormone binding protein are purified enabling amino acid sequence and DNA isolates coding for growth hormone receptor and growth hormone binding protein and methods of obtaining such DNA are provided, together with expression systems for recombinant production of growth hormone receptor and growth hormone binding protein. Therapeutically useful forms of the growth hormone receptor and growth hormone binding protein and anti-receptor antibodies are described.
专利号:US-7161024-B2 优先权日:2003-07-10 标题 :Process for the preparation and purification of 2-(alkoxyalkylidene)-3-ketoalkanoic acid esters from 3-ketoalkanoic acid esters 发明人:DRAPER RICHARD W 权利人:SCHERING CORP 摘要:In its several embodiments, this invention discloses a novel process to prepare the compounds of Formula 3: n nwherein R 1 is lower alkyl, and R 2 and R 3 can be the same or different, each being independently selected from the group consisting of alkyl, aryl and aralkyl; said process being carried out in a suitable solvent with at least one tert-amine carboxylate salt catalyst. The compounds of formula 3 are chemical intermediates useful for the synthesis of various heterocyclic compounds. These heterocyclic compounds are in turn useful precursors for diverse pharmaceutical, herbicidal and insecticidal agents. In particular, these intermediates are useful precursors to a variety of CCR5 inhibitors.
[参考文献]: Katz Ba, Et Al. Structural Basis For Selectivity Of A Small Molecule, S1-Binding, Submicromolar Inhibitor Of Urokinase-Type Plasminogen Activator. Chem Biol. 2000 Apr;7(4):299-312. [参考文献]: Tanizawa K, Et Al. Proteolytic Enzymes. Vi. Aromatic Amidines As Competitive Inhibitors Of Trypsin. J Biochem. 1971 May;69(5):893-9. [参考文献]: Ashwini K Devkota, Et Al. Reversible Covalent Inhibition Of Eef-2K By Carbonitriles. Chembiochem. 2014 Nov 3;15(16):2435-42. [参考文献]: B S Margulies, Et Al. Ewing'S Sarcoma Of Bone Tumor Cells Produces Mcsf That Stimulates Monocyte Proliferation In A Novel Mouse Model Of Ewing'S Sarcoma Of Bone. Bone. 2015 Oct:79:121-30. [参考文献]: David J Busch, Et Al. Intrinsically Disordered Proteins Drive Membrane Curvature. Nat Commun. 2015 Jul 24:6:7875.
合成参考文献
摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 124. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 117. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 190. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 164. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 140.