215927-34-7Relevant academic research and scientific papers
Novel Solid-phase and solution-phase synthetic methods for trisubstituted Thieno[3,2-d]pyrimidine derivatives
Jeon, Moon-Kook,Kim, Jung-Gyu,Lee, Duck-Hyung
supporting information, p. 1406 - 1414 (2016/10/12)
The coupling of 7-aryl-3,4-dihydro-4-oxothieno[3,2-d]pyrimidine-2-carboxylic acid with a primary alkylamineloaded acid-sensitive methoxy benzaldehyde (AMEBA) resin, a benzotriazol-1-yloxytris(dimethylamino) phosphonium hexafluorophosphate (BOP)-mediated amination reaction, and cleavage from the solid support yielded N-alkyl-4-(alkylamino)-7-arylthieno[3,2-d]pyrimidine-2-carboxamide derivatives. The progress of the reactions on solid phase was monitored through attenuated total reflectance-FTIR spectroscopy and was compared with representative solution-phase surrogates. Additionally, N-acylation (acid chloride, InF3 , CH3 CN, room temperature) and cyclization (DBN, 1,4-dioxane, 80 ° C) of a 3-amino-4-(4-t-butoxycarbonylphenyl) thiophene-2-carboxamide intermediate under previously unreported conditions provided 2-substituted thieno[3,2-d]pyrimidin-4(3H)-one derivatives, which were subsequently converted to 2-substituted 4-alkylamino-7-[4-(alkylaminocarbonyl)phenyl]thieno[3,2-d]pyrimidine derivatives through a reaction sequence consisting of a BOP-mediated amination reaction, t-butyl deprotection, and amide formation.
PYRIMIDO-DIAZEPINONE COMPOUND
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Paragraph 0138, (2014/04/03)
Provided are a compound represented by general formula (I), or the pharmaceutically acceptable salt thereof, (wherein Ra represents a hydrogen atom or the like, R1 and R2 may be the same or different, and each represents a hydrogen atom, optionally substituted lower alkyl or cycloalkyl, or R1 and R2 are combined together with the adjacent nitrogen atom thereto to form nitrogen-containing heterocyclic group, and Z represents a bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other, or the like) and the like.
