70558-11-1

Usage

Uses

Used in Pharmaceutical Research and Development:
6-CHLORO-3,4-DIHYDRO-2H-BENZO[1,4]OXAZINE HYDROCHLORIDE is used as a research compound for its potential therapeutic applications in the pharmaceutical industry. It is valued for its potential biological activity, which is currently being explored for the development of new drugs and therapies.
Used in Synthesis of Pharmaceutical Compounds:
In the chemical synthesis industry, 6-CHLORO-3,4-DIHYDRO-2H-BENZO[1,4]OXAZINE HYDROCHLORIDE is used as a key building block. Its role in the synthesis of various pharmaceutical compounds makes it a crucial component in the creation of new medicinal agents, contributing to the advancement of healthcare solutions.

Upstream product

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Relevant academic research and scientific papers

Design, synthesis, and bioevaluation of substituted phenyl isoxazole analogues as herbicide safeners

Herbicide safeners enhance herbicide detoxification in crops without affecting target weed sensitivity. To enhance crop tolerance to the toxicity-related stress caused by the herbicide acetochlor (ACT), a new class of substituted phenyl isoxazole derivatives was designed by an intermediate derivatization method as herbicide safeners. Microwave-assisted synthesis was used to prepare the phenyl isoxazole analogues, and all of the structures were confirmed via IR, 1H NMR, 13C NMR, and HRMS. Compound I-1 was further characterized by X-ray diffraction analysis. Bioassay results showed that most of the obtained compounds provided varying degrees of safening against ACT-induced injury by increasing the corn growth recovery, glutathione content, and glutathione S-transferase activity. In particular, compound I-20 showed excellent safener activity against ACT toxicity, comparable to that of the commercial safener benoxacor. Gaussian calculations have been performed and the results indicated that the nucleophilic ability of compound I-20 is higher than that of benoxacor, thus the activity is higher than that of benoxacor. These findings demonstrate that phenyl isoxazole derivatives possess great potential for protective management in cornfields.

DIHYDRO 1,4-BENZOXAZINES AND METHOD OF SYNTHESIZING THE SAME USING SULFONIUM SALTS

Exemplary embodiments of the present invention relate to benzoxazines having various N-protecting groups. An R1 functional group is at least one selected from the group consisting of H and a halogen, an R2 functional group is at least one selected from the group consisting of H, an amide, or a carbamate, and a Z functional group is at least one selected from the group consisting of a phenyl, substituted phenyl group, methyl, and t-butyl group. The exemplary embodiments provide compounds with benzoxazines having various cleavable protecting groups such as amides and carbamates.

Simple and efficient synthesis of novel N -dichloroacetyl-3,4-dihydro-2 H -1,4-benzoxazines

An easy synthetic route to N -dichloroacetyl- 3,4-dihydro-2 H -1,4-benzoxazine derivatives 3 involves cyclization of 2-aminophenols 1 with 1,2-dibromoethane and subsequent acylation of the resultant 3,4-dihydro- 2 H -1,4-benzoxazine derivatives 2 with dichloroacetyl chloride. All compounds were characterized by IR, 1 H NMR, 13 C NMR, ESI-MS and elemental analysis. The structure of 3a was determined by X-ray crystallographic analysis.

Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds

[Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.

Production Method of Nitrogen-Containing Fused Ring Compounds

[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.

FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS

A series of 5,5-dimethyl-5,6-dihydro-1,3-benzothiazol-7(4H)-one and 7,7-dimethyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[5,4-c]azepin-4-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted benzofused mor

Nitrogen-containing fused ring compounds and use thereof

A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]: wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.

Synthesis of substituted 4-(3-alkyl-1,2,4-oxadiazol-5-ylmethyl)-3,4-dihydro-2H-1,4-benzoxazines and 4-(1H-benzimidazol-2-ylmethyl)-3,4-dihydro-2H-1,4-benzoxazines

Substituted 2H-1,4-benzoxazines were synthesized from substituted 2-amino phenols and 1,2-dibromoethane using K2CO3 in good to excellent yields. The cyclized products were further reacted with alkyl bromides to obtain the desired N-substituted 3,4-dihydro-2H-1,4-benzoxazines.

HETEROARYL SULFONAMIDES AND CCR2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Phenylaminopropanol derivatives and methods of their use

The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.