77956-92-4Relevant academic research and scientific papers
A method for preparing ilastatin is disclosed. Preparation method of intermediate and intermediate
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Paragraph 0048-0050, (2021/10/27)
The preparation method comprises the following steps: (1) the first intermediate 3 - (dimethylamino) methyl) benzofuran -2 - carboxylic acid and second intermediate 4 - (2 - aminoethoxy) methyl benzoate are subjected to amide condensation to obtain third
Benzo-five-membered heterocycle HPPD inhibitor or salt thereof, herbicide composition, preparing method and application
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Paragraph 0040-0045, (2019/10/22)
The invention discloses a benzo-five-membered heterocycle HPPD inhibitor or a salt thereof with a formula I or II, a herbicide composition, a preparing method and application. X in the formula I or IIrepresents a nitrogen atom, an oxygen atom or a sulphur atom; R1 represents a hydrogen atom, C1-6 alkyl, C1-6 alkoxy and aromatic groups; R2 and R3 represent halogen, nitryl, trifluoromethyl, cyano group, sulfone methyl, C1-6 alkyl or C1-6 alkoxy; R4 in the formula I represents a hydrogen atom or methyl; R4 in the formula II represents a hydrogen atom, cyclopropyl, trifluoromethyl, C1-6 alkyl orC1-6 alkoxy; R5 in the formula II represents a hydrogen atom, C1-6 alkyl, C1-6 alkoxy or aromatic rings. According to the benzo-five-membered heterocycle HPPD inhibitor or the salt thereof with the formula I or II, the herbicide composition, the preparing method and application, an organic framework completely different from those of marketized HPPD inhibitors is constructed, and the bioassay activity is equivalent to that of mesotrione. When the inhibitor is used as a herbicide, the growth inhibition effect is significant.
TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS
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Page/Page column 95, (2014/09/29)
The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
1-Benzoxepin-5 (2H)-one derivatives and pharmaceutical compositions
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, (2008/06/13)
Novel, 3-amino-1-benzoxepin-5 (2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: STR1 wherein: R1 and R2 independently of one another are hydrogen, C1 -C5 alkyl, C1 -C5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group, C2 -C5 alkyl substituted with terminal hydroxy or methoxy or, C3 -C4 alkenyl; or one of R1 and R2 are hydrogen or a C1 -C5 alkyl and the other is a C2 -C5 alkyl substituted with a terminal NR5 R6 ; R5 and R6 independently of one another are hydrogen or C1 -C5 alkyl; or R5 and R6 are together a 5 to 7 member ring, or R5 and R6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen; R1 and R2 are together a 5 to 7 member ring, or R1 and R2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR7 ; R7 is hydrogen, methyl, benzyl or phenyl; R3 and R4 independently of one another are hydrogen, halogen, C1 -C4 alkyl, C1 -C4 alkoxy or C1 -C4 alkylthio; or one of R3 and R4 is trifluoromethyl or nitro and the other is hydrogen; and the acid addition salts thereof. These compounds have a favorable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of disorders of the stomach and intestinal tract. Processes for the preparation of the derivatives and their acid addition salts and intermediate products for their preparation are also descrived.
