4318-37-0Relevant articles and documents
GPR139 RECEPTOR MODULATORS
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Page/Page column 165-166, (2020/06/01)
Compounds are provided that modulate the GPR139 receptor, compositions containing the same, and to methods of their preparation and use for treatment of a malcondition wherein modulation of the GPR139 receptor is medically indicated or beneficial. Such compounds have the structure of Formula (X) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R1, R2, R3, R4, R9, R10, R11, and R12, Q5, Q6, Q7 and Q8 are as defined herein.
A BEt3-Base catalyst for amide reduction with silane
Yao, Wubing,Fang, Huaquan,He, Qiaoxing,Peng, Dongjie,Liu, Guixia,Huang, Zheng
, (2019/05/22)
Reported herein is the development of a simple but practical catalytic system for the selective reduction of amides with hydrosilane or hydrosiloxane. Low-cost and readily available triethylborane (1.0 M in THF), in combination with a catalytic amount of an alkali metal base, was found to catalyze the reduction of all three amide classes (tertiary, secondary, and primary amides) to form amines under mild conditions. In addition, the selective transformation of secondary amides to aldimines and primary amides to nitriles can also be achieved by using a proper combination of BEt3 and base. The scope of these BEt3-base-catalyzed amide hydrosilylation reactions has been explored in depth. Preliminary results of mechanistic studies suggest a modified Piers' silane Si-H···B activation mode wherein the hydride abstraction by BEt3 is promoted by the coordination of an alkoxide or hydroxide anion to the Si center.
A BEt3-Base Catalyst for Amide Reduction with Silane
Yao, Wubing,Fang, Huaquan,He, Qiaoxing,Peng, Dongjie,Liu, Guixia,Huang, Zheng
, p. 6084 - 6093 (2019/05/24)
Reported herein is the development of a simple but practical catalytic system for the selective reduction of amides with hydrosilane or hydrosiloxane. Low-cost and readily available triethylborane (1.0 M in THF), in combination with a catalytic amount of an alkali metal base, was found to catalyze the reduction of all three amide classes (tertiary, secondary, and primary amides) to form amines under mild conditions. In addition, the selective transformation of secondary amides to aldimines and primary amides to nitriles can also be achieved by using a proper combination of BEt3 and base. The scope of these BEt3-base-catalyzed amide hydrosilylation reactions has been explored in depth. Preliminary results of mechanistic studies suggest a modified Piers' silane Si-H···B activation mode wherein the hydride abstraction by BEt3 is promoted by the coordination of an alkoxide or hydroxide anion to the Si center.
Process for preparing N-methyl homopiperazine from 2-haloethylamine compound
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Paragraph 0094-0096, (2017/12/27)
The invention discloses a process for preparing N-methyl homopiperazine from 2-haloethylamine compound, and the process comprises the following steps: Step 1, taking the 2-halogenated ethylamine compound as a raw materia to react with ethyl trifluoroacetate to obtain N-(2-Haloethyl) trifluoroacetamide; Step (2) taking the N-(2-Haloethyl) trifluoroacetamide as a raw material to react with methylamine or methylamine hydrochloride to obtain N-methyl-N'-trifluoroacetyl ethylenediamine; Step (3) taking the N-methyl-N'-trifluoroacetyl ethylenediamine as a raw material to react with 1,3-disubstituted propane compound to obtain N-methyl-N'-trifluoroacetyl homopiperazine; Step (4) taking the N-methyl-N'-trifluoroacetyl homopiperazine as a raw material to react with a hydrogen chloride ethanol solution to obtain N-methyl homopiperazine dihydrochloride; and Step (5) taking the N-methyl homopiperazine dihydrochloride as a raw material to prepare the N-methyl homopiperazine by alkalization. The process has the advantages of simple operation, low cost, high yield, low pollution and suitability for industrialized production.
14-substituted marcfortines and derivatives useful as antiparasitic agents
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, (2008/06/13)
There are disclosed 14α-hydroxymarcfortine derivatives of the natural products marcfortine A, B, C, and D useful in the treatment and prevention of helminth and arthropod infections of animals and plants. The synthetic derivatives are of Formula (I). STR1
Marcfortine/paraherquamide derivatives useful as antiparasitic agents
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, (2008/06/13)
There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants. Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.
Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
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, (2008/06/13)
This invention relates to compounds of Formula I STR1 which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.
Antiatherosclerotic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones
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, (2008/06/13)
This invention relates to compounds of Formula I STR1 which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.
Treatment of atherosclerosis with khellin-related furochromones
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, (2008/06/13)
The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
Antiatherosclerotic furochromones
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, (2008/06/13)
The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.