2703-17-5Relevant articles and documents
Functionalization of 2-Trifluoromethyl-1H-pyrrole: A Convenient Entry into Advanced Fluorinated Building Blocks Including all Isomeric 2-(Trifluoromethyl)prolines
Hys, Vasyl Yu.,Shevchuk, Oleksandr I.,Vashchenko, Bohdan V.,Karpenko, Oleksandr V.,Gorlova, Alina O.,Grygorenko, Oleksandr O.
, p. 3896 - 3905 (2020)
The synthetic utility of 2-trifluoromethyl-1H-pyrrole as a pharmaceutically relevant platform was demonstrated by the preparation of mono- and bifunctional C-2(5)- or C-3-substituted derivatives, i.e. regioisomeric sulfonyl halides, carboxylic acids, aldehydes, and nitriles. A series of modifications relied on lithiation or electrophilic substitution, which proceeded regioselectively on multigram scale, mostly in protecting-group-free mode. Subsequent catalytic hydrogenation of the pyrrole ring was also performed for synthesis of all isomeric 2-trifluoromethyl α- and β-prolines. These derivatives were considered as promising low-molecular-weight building blocks for synthesis, drug discovery, and agrochemistry.
IMPROVED METHODS, KITS, COMPOSITIONS AND DOSING REGIMENS FOR THE USE OF HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2
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Page/Page column 101-102, (2021/05/07)
The present application provides improved compositions, methods, kits and dosing regimens for the use of heterocyclic compounds and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, or stereoisomers thereof. These compositions, methods, kit
SULFONAMIDE COMPOUNDS AND THE USE THEREOF IN THE TREATMENT OF CANCER
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Paragraph 00181, (2021/04/23)
The present disclosure relates generally to a class of sulfonamide-based compounds, compositions containing the same and the therapeutic use of the compounds in the treatment of cancer.
Metal-Free Directed C?H Borylation of Pyrroles
Wang, Zheng-Jun,Chen, Xiangyang,Wu, Lei,Wong, Jonathan J.,Liang, Yong,Zhao, Yue,Houk, Kendall N.,Shi, Zhuangzhi
supporting information, p. 8500 - 8504 (2021/03/16)
Robust strategies to enable the rapid construction of complex organoboronates in selective, practical, low-cost, and environmentally friendly modes remain conspicuously underdeveloped. Here, we develop a general strategy for the site-selective C?H borylation of pyrroles by using only BBr3 directed by pivaloyl groups, avoiding the use of any metal. The site-selectivity is generally dominated by chelation and electronic effects, thus forming diverse C2-borylated pyrroles against the steric effect. The formed products can readily engage in downstream transformations, enabling a step-economic process to access drugs such as Lipitor. DFT calculations (wB97X-D) demonstrate the preferred positional selectivity of this reaction.
NOVEL OXADIAZOLE COMPOUNDS CONTAINING 5- MEMBERED HETEROAROMATIC RING FOR CONTROLLING OR PREVENTING PHYTOPATHOGENIC FUNGI
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Page/Page column 74, (2021/02/26)
The present invention relates to a compound of formula (I), wherein, R1,A, A5, A6, A7, A8, R12, n and Q are as defined in the detailed description and a process for preparing the compound of formula (I).The present invention also relates to a method for controlling or preventing phytopathogenic fungi.
COMPOUNDS AND USES THEREOF
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Page/Page column 150, (2020/08/22)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
Preparation method of 4-ethyl-1H-pyrrole-3-methyl carboxylate
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Paragraph 0013-0015, (2019/08/30)
The invention discloses a preparation method of 4-ethyl-1H-pyrrole-3-methyl carboxylate, and belongs to the field of chemical engineering. The preparation method comprises following steps: 3-pyrrole methyl carboxylate preparation: taking concentrated sulfuric acid as a catalyst, adding 3-pyrrole carboxylic acid into a methanol solution, carrying out reactions for 2 to 4 hours at a temperature of 45 to 65 DEG C, continuously extracting 3-pyrrole methyl carboxylate to obtain 3-pyrrole methyl carboxylate according to the reaction balance principle; taking a mixture composed of anhydrous calcium chloride and nano alumina as a catalyst, heating to a temperature of 80 to 100 DEG C, adding ethane, stirring for 40 to 60 minutes, cooling to a temperature of 5 to 10 DEG C, allowing the system to stand still for 12 to 14 hours, subjecting the reaction liquid to vacuum concentration, re-crystallizing obtained solids in a mixed solvent, which is composed of ether and ethane according to a volume ratio of 1:1-2; and drying to obtain 4-ethyl-1H-pyrrole-3-methyl carboxylate. The preparation is simple, the method and principle are reasonable, and the preparation method is suitable for popularization and application.
HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 0459-0460, (2017/01/02)
The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a
Beneficial Effects of Electrochemistry in Cross-Coupling Reactions: Electroreductive Synthesis of 4-Aryl- or 4-Heteroaryl-6-pyrrolylpyrimidines
Sengmany, Stéphane,Vasseur, Stéphane,Lajnef, Abdelmoumen,Le Gall, Erwan,Léonel, Eric
supporting information, p. 4865 - 4871 (2016/10/13)
The rarely described 4-(hetero)aryl-6-pyrrolylpyrimidines are prepared by electroreductive nickel-catalysed cross-coupling reactions between aryl halides and chloropyrimidines. Inherent predictable issues of such metal-catalysed reactions that involve or
Proton pump inhibitors
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Paragraph 0213, (2015/11/16)
A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R 1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R 2 , R 3 and R 4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R 5 and R 6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.