5-氰基-1H-吲哚-2-羧酸乙酯置于calcium Oxide体系中,化学反应生成5-氰基吲哚 参考文献:Synthesis And Reactions Of Indole Carboxylic Acids; Pyridindolones From Indole-2-Carboxyacetalylbenzylamides 标题:Synthesis And Reactions Of Indole Carboxylic Acids; Pyridindolones From Indole-2-Carboxyacetalylbenzylamides 摘要: Doi:10.1021/jo01132A001
专利号:US-9394264-B2 优先权日:2009-11-13 标 题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA 权利人:RECEPTOS INC 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-3992392-A 优先权日:1973-04-27 标题:Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an N-haloaniline with a β-carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the β-carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an α-ethyl-β -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:US-2014275542-A1 优先权日:2013-03-15 标 题 :Synthesis of a serotonin reuptake inhibitor 发明人:TADDEI MAURIZIO; GIANNOTTI LUCA; ATTOLINO EMANUELE; ALLEGRINI PIETRO 权利人:DIPHARMA FRANCIS SRL 摘要:Process for the preparation of a piperazinyl derivative, and its intermediates, which has known activity as a serotonin reuptake inhibitor and is used in therapy for treating serious symptoms of depression in adults.
专利号:US-10752927-B2 优先权日:2018-03-01 标 题 :Method for the synthesis of tryptophan analogs in aqueous solvents at reduced temperatures 发明人:BOVILLE CHRISTINA E; ROMNEY DAVID K; ALMHJELL PATRICK J; SIEBEN MICHAELA M 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure provides methods for preparing tryptophans and tryptophan derivatives. The methods include: combining i) an indole substrate or azulene substrate, ii) a serine substrate, and iii) an engineered tryptophan synthase β-subunit (TrpB); and maintaining the resulting mixture under conditions sufficient to form the product compound. The engineered TrpB comprises a PLP binding loop mutation, a helix 1 mutation, a strand 7-8 mutation, or a combination thereof. New TrpB variants are also described.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-2019271016-A1 优先权日:2018-03-01 标题:Method for the synthesis of tryptophan analogs in aqueous solvents at reduced temperatures
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