6228-73-5Relevant articles and documents
Novel method and technology for synthesizing cyclopropyl ammonia
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Paragraph 0018, (2021/09/21)
The invention discloses a synthesis process route of a cyclopropane synthetic route. In the process route, cyanocyclopropane 1 - formic acid (-1 -) and (1) are subjected to hydrolysis under the action of a strong base to generate 1-cyanocyclopropane 1 - formic acid (-1 -), (2) decarboxylation to generate cyclopropanecarboxamide (2 3), and (4 4 3) subjected to Hoffman rearrangement to obtain the target product cyclopropysite. The process route is longer than the production process in the present stage, the reaction route is long, the use of high-temperature and high-pressure is avoided, the danger is reduced, and the safety is improved. The requirement of the reaction equipment is reduced, the used raw materials are easy to obtain, operation is easy, safety and environmental protection are achieved, and industrial production can be realized.
Modular Continuous Flow Synthesis of Imatinib and Analogues
Fu, Wai Chung,Jamison, Timothy F.
supporting information, p. 6112 - 6116 (2019/08/26)
A modular continuous flow synthesis of imatinib and analogues is reported. Structurally diverse imatinib analogues are rapidly generated using three readily available building blocks via a flow hydration/chemoselective C-N coupling sequence. The newly developed continuous flow hydration and amidation modules each exhibit a broad scope with good to excellent yields. Overall, the method described does not require solvent switches, in-line purifications, or packed-bed apparatuses due to the judicious manipulation of flow setups and solvent mixtures.
Efficient Hydration of Nitriles Promoted by Gallic Acid Derived from Renewable Bioresources
Deng, Tao,Wang, Cheng-Zhang
, p. 1349 - 1353 (2017/04/14)
An efficient gallic acid promoted nitriles hydration at room temperature with ethanol/water as a solvent has been developed. The present protocol offers a wide range of amides in moderate to good yields. Moreover, galla chinensis extract can serve as the promoter to perform the hydration, which also shows the potential utilization of natural feedstocks.
Method for preparing amide by metallic sodium catalyzed ester ammonolysis reaction
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Paragraph 0066, (2017/08/30)
The invention discloses a method for preparing amide by metallic sodium catalyzed ester ammonolysis reaction. The method is characterized in that ester and liquid ammonia are taken as raw materials, and metallic sodium is taken as a catalyst to perform reaction at a temperature of 90-140 DEG C in a high-pressure kettle; a molar ratio of the ester to ammonium is 1: (1.2 to 5.0); molar weight of the metallic sodium is 4-10% that of the ester; when reaction pressure is not lowered any longer, reaction is stopped to recycle the ammonium which is not reacted; and an obtained reaction product is post-treated to obtain a product. The method can be used for efficiently preparing the amide; and moreover, the raw materials are cheap and are low in toxicity, reaction activity is relatively high, dose of the catalyst is small, reaction speed is high, a reaction conversion rate is high, and the product is easily separated.
Corresponding amine nitrile and method of manufacturing thereof
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Paragraph 0133-0136; 0165-0169; 0199-0202, (2017/10/22)
The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
Clean synthesis of primary to tertiary carboxamides by CsOH-catalyzed aminolysis of nitriles in water
Li, Yang,Chen, Haonan,Liu, Jianping,Wan, Xujun,Xu, Qing
supporting information, p. 4865 - 4870 (2016/10/06)
Using CsOH as the only catalyst and utilizing its "cesium effect", a clean synthesis of a wide range of primary, secondary, and tertiary carboxamides was achieved by aminolysis reactions of nitriles with ammonia, primary, or secondary amines in water. Studies on the control reactions revealed that the reactions with ammonia most probably proceed via an aminolysis path by the initial addition of ammonia to Cs-activated nitriles to form unsubstituted amidine intermediates, while the reactions with primary or secondary amines may proceed via a hydration/transamidation path by the initial hydration of the Cs-activated nitriles to form primary carboxamide intermediates followed by their transamidation with amines through the formation of substituted amidine intermediates.
Efficient and selective nitrile hydration reactions in water catalyzed by an unexpected dimethylsulfinyl anion generated in situ from CsOH and DMSO
Chen, Haonan,Dai, Wujie,Chen, Yi,Xu, Qing,Chen, Jianhui,Yu, Lei,Zhao, Yajuan,Ye, Mingde,Pan, Yuanjiang
supporting information, p. 2136 - 2141 (2014/04/17)
Unexpected dimethylsulfinyl anions (I), generated in situ from the superbase system CsOH-DMSO, was found to be a highly active catalyst for controllable nitrile hydration reactions in water, which selectively afforded the versatile amides via interesting Cs-activated I-catalyzed direct and indirect hydration mechanisms involving an O-transfer process from DMSO onto the nitriles. the Partner Organisations 2014.
HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0365, (2014/06/23)
The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A′ B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 59-60, (2012/12/13)
The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A' B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
1,2-DISUBSTITUTED CYCLOPROPANES
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, (2008/06/13)
Compounds of Formula I wherein the substituents are as described in the specification or pharmaceutically acceptable salts or stereochemically isomeric forms thereof, useful for treating diseases related to calcium imbalance and metabolism.
