2,6-二硝基甲苯置于ammonium Hydroxide,硫化氢体系中,用 乙醇 作为反应溶剂,化学反应生成 2-甲基-3-硝基苯甲醚 参考文献:ber Die Konstitution Eines Nebenalkaloides Aus Adhatoda Vasica Nees 标题:ber Die Konstitution Eines Nebenalkaloides Aus Adhatoda Vasica Nees 摘要: DOI:10.1007/bf00899842
专利号:US-4013664-A 优先权日:1973-06-20 标 题:Synthesis of hernandaline 发明人:KUPCHAN S MORRIS; KAMESWARAN VENKATARAMAN 权利人:RESEARCH CORP 摘要:There is disclosed a novel and improved method of synthesizing aporphines utilizing the Pschorr cyclization of 1-(2'-aminobenzyl)-7 hydroxy-1,2,3,4-tetrahydroisoquinolines in place of the corresponding 7-methoxy compounds. n In the novel process of the present invention the amino group is diazotized and cyclized in the presence of copper powder.
专利号:WO-0144184-A1 优先权日:1999-12-16 标题:Synthesis of indole-containing spla2 inhibitors 发明人:MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT 权利人:LILLY CO ELI; MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT 摘要:A method of making a compound include reacting a compound represented by formula (I), with a base, to form the compound of formula (II); and where R1 is H, R10 or -C(O)R10; R2 is R20 -OR20, -SR20, -NR20R20' or -C(O)R20;R3, R4, R5, R6 and R7 are each individually H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R or -S(O)2R; provided that at least one of R4 and R5 is not H; each R, R10 and R20 is individually alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and W is a trisubstituted phosphorous. The method provides an alternative route to indole-3-glyoxylamide compounds.
专利号:WO-9729091-A1 优先权日:1996-02-09 标题:Balanol analogues 发明人:NIELSEN JOHN; LYNGSOE LARS OLE 权利人:AUDA PHARMACEUTICALS APS; NIELSEN JOHN; LYNGSOE LARS OLE 摘要:The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.