1452-16-0Relevant articles and documents
Preparation method of medicinal intermediate 2-cyanothiazole
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Paragraph 0017-0024, (2019/03/08)
The invention provides a preparation method of medicinal intermediate 2-cyanothiazole. The preparation method comprises the steps that in a reaction container, N-methylimidazole serves as a reaction solvent, CuI serves as a catalyst, K4[Fe(CN)6] and 2-bro
Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C2and C6positions
Oh, Changmok,Kim, Hyuntae,Kang, Jong Soon,Yun, Jieun,Sim, Jaejun,Kim, Hwan-Mook,Han, Gyoonhee
, p. 496 - 500 (2017/01/16)
Acute myeloid leukemia (AML) is a clonal disorder of hematopoietic progenitor cell. In AML, a mutation in FLT3 is commonly occurs and is associated with poor prognosis. We have previously reported that thieno[2,3-d]pyrimidine derivative compound 1 exhibited better antiproliferative activity against MV4-11 cells which harbor mutant FLT3 than AC220, which is a well-known FLT3 inhibitor, and has good microsomal stability. However, compound 1 had poor solubility. We then carried out further structural modification at the C2and the C6positions of thieno[2,3-d]pyrimidine scaffold. Compound 13b, which possesses a thiazole moiety at the C2position, exhibited better antiproliferative activity than compound 1 and showed increased solubility and moderate microsomal stability. These results indicate that compound 13b could be a promising potential FLT inhibitor for AML chemotherapy.
Synthesis of nitriles from aldehydes with trimethylphenylammonium tribromide and ammonium acetate
Sayama, Shinsei
, p. 1796 - 1802 (2016/11/06)
Various aromatic and heterocyclic aldehydes were easily converted to respective nitriles with the combination of trimethylphenylammonium tribromide and ammonium acetate in good yields at room temperature.
COMPOUNDS HAVING AN ETHR INHIBITING ACTIVITY - USE OF SAID COMPOUNDS AS DRUGS - PHARMACEUTICAL COMPOSITION AND PRODUCT CONTAINING SAID COMPOUNDS
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Page/Page column 11, (2013/05/21)
The present invention relates to compounds of Formula (I), wherein R1 is chosen among the following radicals : (II); (III); (IV), (V), (VI) (VII) and n= 1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is (VIII). The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis.
Schmidt reaction in ionic liquids: Highly efficient and selective conversion of aromatic and heteroaromatic aldehydes to nitriles with [BMIM(SO3H)][OTf] as catalyst and [BMIM][PF6] as solvent
Nandi, Ganesh C.,Laali, Kenneth K.
, p. 2177 - 2179 (2013/04/24)
A mild and selective method is presented for the conversion of aromatic and heteroaromatic aldehydes to nitriles via the Schmidt reaction with TMSN 3 by using [BMIM(SO3H)][OTf] as catalyst and [BMIM][PF6] as solvent. The method offers high yields and simple product isolation, and avoids the use of liquid superacids or corrosive Lewis acids commonly employed for this transformation. It also offers some potential for recycling/reuse of the IL solvent.
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors
Flipo, Marion,Desroses, Matthieu,Lecat-Guillet, Nathalie,Villemagne, Baptiste,Blondiaux, Nicolas,Leroux, Florence,Piveteau, Catherine,Mathys, Vanessa,Flament, Marie-Pierre,Siepmann, Juergen,Villeret, Vincent,Wohlk?nig, Alexandre,Wintjens, René,Soror, Sameh H.,Christophe, Thierry,Jeon, Hee Kyoung,Locht, Camille,Brodin, Priscille,Déprez, Benoit,Baulard, Alain R.,Willand, Nicolas
experimental part, p. 68 - 83 (2012/03/10)
Mycobacterial transcriptional repressor EthR controls the expression of EthA, the bacterial monooxygenase activating ethionamide, and is thus largely responsible for the low sensitivity of the human pathogen Mycobacterium tuberculosis to this antibiotic.
PTERIDINONES AS INHIBITORS OF POLO - LIKE KINASE
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Page/Page column 105; 106, (2011/07/09)
The present invention provides compounds having a structure according to Formula (I) or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
METHYLENE AMINES OF THIENO [2,3-D] PYRIMIDINE AND THEIR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS
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Page/Page column 57, (2010/04/30)
This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R1 and R2 are definedin the specification. Disorders treated and/or prevented include Parkinson's Disease.
Process for catalytically preparing aromatic or heteroaromatic nitriles
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Page/Page column 4, (2009/04/24)
The present invention relates to a process for preparing optionally substituted aromatic or heteroaromatic nitriles starting from haloaromatics. These are reacted in a copper-catalysed reaction with potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III) in the presence of heteroaromatic amines.
A bio-inspired copper catalyst system for practical catalytic cyanation of aryl bromides
Schareina, Thomas,Zapf, Alexander,Cotte, Alain,Mueller, Nikolaus,Beller, Matthias
experimental part, p. 3351 - 3355 (2009/06/06)
A general and environmentally improved protocol for the cyanation of aryl halides with the nontoxic cyanide source potassium hexacyanoferrate(II) {K 4[Fe(CN)6]} using copper catalysis and a ligand system based on 1-alkyl-1H-imidazoles is presented. The advantages of this system are a wide substrate range, high selectivity, easy handling, and inexpensive reagents.
