116457-91-1Relevant articles and documents
Copper(I)-Mediated Denitrogenative Macrocyclization for the Synthesis of Cyclic α3β-Tetrapeptide Analogues
Chen, Chun-Chi,Wang, Sheng-Fu,Su, Yung-Yu,Lin, Yuya A.,Lin, Po-Chiao
, p. 1326 - 1337 (2017)
A copper(I)-mediated denitrogenative reaction has been successfully developed for the preparation of cyclic tetrapeptides. The key reactive intermediate, ketenimine, triggers intramolecular cyclization through attack of the terminal amine group to generate an internal β-amino acid with an amidine linkage. The chemistry developed herein provides a new synthetic route for the preparation of cyclic α3β-tetrapeptide analogues that contain important biological properties and results in rich structural information being obtained for conformational studies. With the success of this copper(I)-catalyzed macrocyclization, two histone deacetylase inhibitor analogues consisting of the cyclic α3β-tetrapeptide framework have been successfully synthesized.
Method for catalyzing asymmetric Henry reaction of trifluoromethyl ketone
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Paragraph 0192-0194, (2021/03/06)
The invention provides a method for catalyzing asymmetric Henry reaction of trifluoromethyl ketone. The method adopts a brand-new catalyst namely a compound shown as a formula I, and is simple to operate, high in substrate universality, high in reaction y
BENZOTHIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS
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Paragraph 0719-0721, (2020/08/20)
The invention relates to 1,5-benzothiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also r
Preparation method of 2,3-diamido methyl propionate
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Paragraph 0036; 0039; 0041, (2019/02/04)
The invention provides a preparation method of 2,3-diamido methyl propionate. According to the method, serine is used as a raw material, in methyl alcohol, thionyl chloride is used as a catalyst for preparing serine methylester, then the serine methyleste
Aryl substituted aminotetrahydropyran compound and use thereof
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Paragraph 0368; 0370; 0371, (2019/07/04)
The invention relates to an aryl substituted aminotetrahydropyran compound and use thereof, and further relates to a pharmaceutical composition comprising the compound. The compound or pharmaceuticalcomposition provided by the invention can be used as a dipeptidyl peptidase-IV (DPP-IV) inhibitor.
MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS
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Paragraph 0507, (2019/05/02)
The compounds of the present invention are represented by the following compounds having Formula I and Formula (I'): where the substituents R1, R2, R2', R3, R4, R5, R', R", X, Y, and Z are as defined herein and where the substituents R1, R2, R3, R4, R5, R', R", X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
Highly Chemoselective Deprotection of the 2,2,2-Trichloroethoxycarbonyl (Troc) Protecting Group
Trost, Barry M.,Kalnmals, Christopher A.,Tracy, Jacob S.,Bai, Wen-Ju
supporting information, p. 8043 - 8046 (2019/01/04)
Nonreducing, pH-neutral conditions for the selective cleavage of the 2,2,2-trichloroethoxycarbonyl (Troc) protecting group are reported. Using trimethyltin hydroxide in 1,2-dichloroethane, Troc-protected alcohols, thiols, and amines can be selectively unmasked in the presence of various functionalities that are incompatible with the reducing conditions traditionally used to remove the Troc group. This mild deprotection protocol tolerates a variety of other hydrolytically sensitive and acid/base-sensitive moieties as well.
Activation of Remote meta-C?H Bonds in Arenes with Tethered Alcohols: A Salicylonitrile Template
Zhang, Lanlan,Zhao, Chaoyue,Liu, Yang,Xu, Jiancong,Xu, Xiufang,Jin, Zhong
supporting information, p. 12245 - 12249 (2017/09/06)
Palladium-catalyzed activation of remote meta-C?H bonds in arenes containing tethered alcohols was achieved with high regioselectivity by using a nitrile template. Computational studies on the macrocyclic transition state of the regioselectivity-determini
PHOSPHONATE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS
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Paragraph 0585, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I''' or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit
LZC696 intermediate and synthetic method therefor
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Paragraph 0066; 0067; 0068; 0069, (2016/10/09)
The invention discloses a compound which is (R)-tert-butyl(1,((1,1'biphenyl)-4-yl)3-((t-butyldimethylsilyl)oxo)propane-2-yl)carbamate, and the structural formula of the compound is as shown in formula A in the specification. An LZC696 intermediate is synthetized by adopting the compound, the whole technological process is free of expensive reagents or raw materials, free of sensitive reaction for oxygen and simple in purifying procedure, and commercial using purity can be achieved only by recrystallization purification of the compound 3 and the final product. The synthetic process of the invention is low in cost, simple and environmentally-friendly, and is suitable for industrial mass production.
