- Preparation method of (s)-N-ethyl-2-aminomethylpyrrolidine
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The invention provides a preparation method of (s)-N-ethyl-2-aminomethylpyrrolidine. 2-amino-5-hydroxyvaleric acid used as a raw material undergoes esterification protection to obtain methyl 2-amino-5-hydroxypentanoate, N-ethylation is further achieved through bromoethane, and then the N-ethyl-2-aminomethylpyrrolidine is prepared through hydroxyl halogenation, substitution cyclization, ammonolysisand reduction six-step reaction. High-cost raw materials and an N,O-diethylation reaction are successfully avoided, and the method has the advantages of easiness in implementation of the above reaction route, few byproducts, high yield reaching 64.2%, and suitableness for industrialization.
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Paragraph 0015
(2020/06/05)
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- EPHA4 CYCLIC PEPTIDE ANTAGONISTS AND METHODS OF USE THEREOF
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Disclosed herein are compounds and methods of use thereof for the modulation of EphA4 receptor activity. In an aspect, is provided a method of treating or preventing a disease or disorder mediated by EphA4, comprising administering to a subject in need thereof a therapeutically effective amount of a compound as described herein, including certain embodiments, or the structural Formula (I), (l-A), (II), (III), (IV), (IV-1), (V), (Vl-A), (Vl-B), (VII-1), (VII-2), (VIII-1), or (VIII-2), or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or an isotopic variant thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof.
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Paragraph 0653-0655
(2019/11/19)
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- Synthesis of Lepadiformine Using a Hydroamination Transform
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Dissection of lepadiformine by a double hydroamination transform affords a simple achiral amino diene. This reaction is accomplished in the forward sense by amine-directed hydroboration and an oxidative alkyl shift to nitrogen, both of which occur with hi
- Tabor, M. Greg,Shenvi, Ryan A.
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p. 5776 - 5779
(2015/12/11)
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- Selective reduction of amides to amines by boronic acid catalyzed hydrosilylation
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Not a 'B'ore! Benzothiophene-based boronic acids catalyze the reduction of tertiary, secondary, and primary amides in the presence of a hydrosilane. The reaction demonstrates good functional-group tolerance. Copyright
- Li, Yuehui,Molina De La Torre, Jesus A.,Grabow, Kathleen,Bentrup, Ursula,Junge, Kathrin,Zhou, Shaolin,Brueckner, Angelika,Beller, Matthias
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p. 11577 - 11580
(2013/11/06)
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- SUBSTITUTED BENZAMIDE MODULATORS OF DOPAMINE RECEPTOR
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The present invention relates to new substituted benzamide modulators of dopamine receptor, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 12
(2010/05/13)
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- EFFICIENT STEREOCONSERVATIVE SYNTHESIS OF 1-SUBSTITUTED (S)- AND (R)-2-AMINOMETHYLPYRROLIDINES AND INTERMEDIATES THERETO
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Stereoconservative method for preparation of an (R)- or (S)-isomer of the compound of the formula I with at least 95% optical purity wherein R1 is a hydrogen atom, a saturated or unsaturated lower alkyl group, a cycloalkyl group, or a group (CH2)m Ph wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group including 1) O,N-dialkylation, directly or stepwise of (R)- or (S)-proline 2) aminolysis 3) reduction to formation of the (R)- or (S)-isomer of the compound of the formula I, and new intermediates II and III in optical active form obtained by the reaction steps above and wherein R2 is defined as R1 above.
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