📜N,N-Dibenzylaminoacetonitrile置于lithium Aluminium Tetrahydride体系中,用 乙醚 用作溶剂,化学反应 1.0H,反应生成N,N'-二苄基乙二胺 参考文献:Synthesis And Neuroleptic Activity Of Benzamides. Cis-N-(1-Benzyl-2-Methylpyrrolidin-3-yl)-5-Chloro-2-Methoxy-4-(Methylamino)Benzamide And Related Compounds 标题:Synthesis And Neuroleptic Activity Of Benzamides. Cis-N-(1-Benzyl-2-Methylpyrrolidin-3-yl)-5-Chloro-2-Methoxy-4-(Methylamino)Benzamide And Related Compounds 摘要:Three Series Of Benzamides Of N,N-Disubstituted Ethylenediamines (Linear Alkane-1,2-Diamines),1-Substituted 2-(Aminomethyl)Pyrrolidines,And 1-Substituted 3-Aminopyrrolidines (Cyclic Alkane-1,2-Diamines) Were Designed And Synthesized As Potential Neuroleptics. All Target Compounds Were Evaluated For Their Inhibitory Effects On Apomorphine-Induced Stereotyped Behavior In Rats,And A Good Correlation Between Structure And Activity Was Found Throughout The Series. In The Linear Series (Analogues Of Metoclopramide),Introduction Of A Benzyl Group On The Terminal Nitrogen,Rather Than An Ethyl Group,And A Methyl Group On The P-Amino Group Of Metoclopramide Both Enhanced The Activity. The Resulting N-[2-(N-Benzyl-N-Methylamino)Ethyl]-5-Chloro-2-Methoxy-4-(Methylamino) Benzamide(23) Was About 15 Times More Active Than Metoclopramide. In The Cyclic Series,Particularly Among The Benzamides Of 1-Benzyl-3-Aminopyrrolidine,Most Of The Compounds Tested Were More Active Than The Corresponding Linear Benzamides. Cis-N-(1-Benzyl-2-Methylpyrrolidin-3-yl)-5-Chloro-2-Methoxy-4-(Methylamino) Benzamide (Ym-09151-2,55) Was The Most Active Among All Of The Compounds Tested,Being 13 And 408 Times More Potent Than Haloperidol And Metoclopramide,Respectively. Moreover,Compound 55 Exhibited A Fairly High Ratio Of Antistereotypic Activity To Cataleptogenicity Compared With Haloperidol And Metoclopramide. It Is Expected That Compound 55 May Be Used As A Potent Drug With Few Side Effects In The Treatment Of Psychosis. Doi:10.1021/jm00142A019
专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:WO-2025119975-A1 优先权日:2023-12-04 标 题:A method for synthesis of harmine 发明人:HETT ROBERT; GRAB HANUSCH; LAGOUTTE ROMAN 权利人:RECONNECT LABS AG 摘要:The invention relates to a method of synthesis of a compound of formula (I), harmine, according to the method comprising a step of transforming the compound of formula (II), into the compound of formula (I). The invention further relates to a compound of formula (II), which is an intermediate in synthesis of harmine according to the present invention.
专利号:WO-2024068853-A1 优先权日:2022-09-30 标题 :Improved synthesis of otviciclib 发明人:HUBER LUKAS A; GSTACH HUBERT; MASTALIR MATTHIAS; LEBAN JOHANN 权利人:MEDIZINISCHE UNIV INNSBRUCK 摘要:The present invention relates to an improved synthesis of Otviciclib (N-{4-[l-(2,6-Dichloro-4- sulfamoyl-phenyl)-3-dimethylamino-4-oxo-4,5-dihydro-lH-pyrazolo[3,4-d]pyrimidin-6- ylmethyl]-phenyl}-2-diethylamino-acetamide) and its derivatives, and furthermore relates to intermediates useful in this synthesis.
专利号:US-2024336586-A1 优先权日:2021-07-29 标题:Methods for synthesis of racemic, scalemic, and chiral alpha-tocotrienol quinone 发明人:GIANNOUSIS PETER; MOLLARD PAUL; GOUDEDRANCHE SEBASTIEN; KARASAWA TOMOYA 权利人:PTC THERAPEUTICS INC 摘要:The application discloses methods useful for the synthesis of racemic, scalemic, and chiral alpha-tocotrienol quinone, including synthetic intermediates and methods for making said synthetic intermediates.
专利号:US-2023002312-A1 优先权日:2019-11-20 标题:A continuous flow process for the synthesis of hydroxamic acid 发明人:PIMPALE MILIND JAGANNATH; KINI PRASHANT VASANT 权利人:UPL LTD 摘要:The present invention relates to a process for the synthesis of hydroxamic acids by continuous flow process wherein said process comprising reacting alkyl ester with hydroxyl amine salt in presence of base in a microreactor system and continuously producing hydroxamic acid.
专利号:US-10793495-B2 优先权日:2015-08-14 标 题:Synthesis of polyaryl substituted aryl compounds 发明人:BOULOS RAMIZ; FEUTRILL JOHN 权利人:BOULOS & COOPER PHARMACEUTICALS PTY LTD 摘要:A method for the synthesis of a aryl compound of Formula (1).n nU T-W—R 1 ) n    (1)
参考文献:10.1021/ic030218x 摘要:Chandra T, Allred RA, Kraft BJ, Berreau LM, Zaleski JM. Syntheses and thermal reactivities of tetradentate metalloenediynes of Cu(II) and Zn(II). Inorg Chem. 2004 Jan 26;43(2):411–20. doi: 10.1021/ic030218x.