888731-58-6

Basic information

• Product Name: 5-Methyl-3,4-dihydro-2H-benzo[1,4]oxazine
• Synonyms: 5-Methyl-3,4-dihydro-2H-benzo[1,4]oxazine;5-methyl-3,4-dihydro-2H-benzo[b][1,4]oxazine
• CAS NO: 888731-58-6
• Molecular Formula: C₉H₁₁NO
• Molecular Weight: 149.18974
• Mol File: 888731-58-6.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 5-Methyl-3,4-dihydro-2H-benzo[1,4]oxazine(CAS DataBase Reference)
• NIST Chemistry Reference: 5-Methyl-3,4-dihydro-2H-benzo[1,4]oxazine(888731-58-6)
• EPA Substance Registry System: 5-Methyl-3,4-dihydro-2H-benzo[1,4]oxazine(888731-58-6)

Safety Data

• Hazardous Substances Data: 888731-58-6(Hazardous Substances Data)

Upstream product

• 2835-97-4 2-amino-3-methylphenol 
• 106-93-4 ethylene dibromide 
• 31366-49-1 5-methyl-4H-benzo[1,4]oxazin-3-one 
• 888731-57-5 2-chloro-N-(2-hydroxy-6-methylphenyl)-acetamide 

Downstream Products

• 915160-97-3 (5-methyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-acetic acid benzyl ester 

Relevant articles and documents

COMPOUND HAVING 11 ?-HSD1 INHIBITORY ACTIVITY

The present invention provides compounds having excellent 11β-HSD1 inhibitory activity. A compound represented by the following formula (I): [wherein X1 represents an oxygen atom, or the formula -(CR11R12)p-, etc., Y1 represents a hydrogen atom, a hydroxyl group, etc., Z1 represents an oxygen atom or the formula -(NR14)-, R1 represents a hydrogen atom, a halogen atom, a cyano group, a C1-4 alkyl group, a C1-4 alkyl group substituted with 1 to 3 halogen atoms, a C1-4 alkoxy group, a C1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R2 represents a hydrogen atom or a C1-4 alkyl group, and n represents an integer of 1 or 2].

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.

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.

Reductive N-alkylation of aromatic amines and nitro compounds with nitriles using polymethylhydrosiloxane

The potential utility of polymethylhydrosiloxane (PMHS) as a reducing agent for reductive N-alkylation of aromatic amines and nitro compounds using nitriles as an alkylating agent and Pd(OH)2/C as a catalyst is described. The application of this method for the synthesis of several heterocyclic compounds is also reported.

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.