合成目标产物 (1H-Benzo[d]Imidazol-2-yl)Methanamine 主要起始原料 O-Phenylenediamine And Glycine
(文献来源)合成步骤主要原料 O-Phenylenediamine 和 Glycine
📜2-(Aminomethyl)Benzimidazole Dihydrochloride置于氢氧化钾体系中,用 甲醇 作为反应溶剂,化学反应 0.5H,反应生成 (1H-苯并咪唑-2-亚甲基)胺 参考文献:Benzimidazole Compounds That Are Vitronectin Receptor Antagonists 标题:Benzimidazole Compounds That Are Vitronectin Receptor Antagonists
专利号:US-5569762-A 优先权日:1994-01-14 标题:Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds 发明人:WISSNER ALLAN; TROVA MICHAEL P 权利人:AMERICAN CYANAMID CO 摘要:The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein R 1 , R 50 and Z are described in the specification. The improved process includes either synthesis of diastereomeric iodolactones which are separated prior to conversion to compounds of Formula II or III or synthesis of an epoxide which is converted directly to compounds of Formula II and III.
专利号:WO-9931124-A1 优先权日:1997-12-12 标 题:Cholic acid-based scaffolds for multidimensional molecular presentation of peptides 发明人:HOEEG-JENSEN THOMAS 权利人:NOVO NORDISK AS; HOEEG JENSEN THOMAS 摘要:A solid phase method for the synthesis of a plurality of differently substituted cholic acid scaffolds with a wide variety of peptide chain, pseudo-peptide chain or peptoid chain substitutents, as leads or compounds of potential therapeutic interest. The substituted cholic acids are prepared by initial solution synthesis of a scaffold holding amino acids with 3 orthogonal protecting groups. Subsequent solid-phase synthesis provides the build-up of the target molecules, either as discretes or in mixture. The molecules may be screened on the resin or cleaved from the resin and then screened in solution. The method disclosed here provides an easy and fast access to highly diverse compounds, potential peptide mimetics and potential leads for compounds of therapeutic interest. The method is amenable to automatization.
专利号:US-7186709-B2 优先权日:2002-08-27 标 题:Dihydropyrancarboxamides and uses thereof 发明人:SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN 权利人:HARVARD COLLEGE 摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
专利号:US-7179918-B2 优先权日:2001-06-11 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-9914695-B2 优先权日:2015-07-10 标题:Two-step process for preparing 3-substituted phenylalkylamines 发明人:Teramura Doug; LIAO SUBO 权利人:MALLINCKRODT LLC 摘要:Processes for preparing 3-substituted phenylalkylamines comprising reacting a phenyl boronic compound with an α-β unsaturated carbonyl-containing compound via an asymmetric 1,4-addition reaction, followed by reductive alkylation. The processes may be useful in the synthesis of tapentadol.
专利号:WO-0009116-A1 优先权日:1998-08-14 标 题:Grp receptor ligands 发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.