14847-35-9

Usage

Type of compound

Heterocyclic compound

Structural features

Contains a naphthalene ring and an oxazinone ring

Usage

Commonly used in organic synthesis and pharmaceutical research

Therapeutic activities

Exhibits potential anti-inflammatory and anti-cancer properties

Building block

Used for the synthesis of various pharmacologically active compounds

Other properties

Studied for antimicrobial and antioxidant properties, making it valuable in medicinal and pharmaceutical research.

InChI:InChI=1/C12H9NO2/c14-11-7-15-10-6-5-8-3-1-2-4-9(8)12(10)13-11/h1-6H,7H2,(H,13,14)

Upstream product

• 2834-92-6 1-amino-2-naphthol 
• 79-04-9 chloroacetyl chloride 
• 2246-42-6 2-methoxynaphthylamine 
• 120-23-0 (2-naphthoyl)oxyacetic acid 
• 1198-27-2 1-aminonaphthalene-2-ol hydrochloride 
• 135-19-3 β-naphthol 
• 106475-42-7 chloro-acetic acid-(2-methoxy-[1]naphthylamide) 
• 792931-81-8 chloro-acetic acid-(2-ethoxy-[1]naphthylamide) 
• 6913-45-7 N-(2-hydroxy-1-naphthyl)chloroacetoamide 
• 10440-91-2 (1-nitro-[2]naphthyloxy)-acetic acid 
• 91961-41-0 (1-chloro-[2]naphthyloxy)-acetic acid amide 

Relevant academic research and scientific papers

Efficient synthesis of benzene-fused 6/7-membered amides: Via Xphos Pd G2 catalyzed intramolecular C-N bond formation

An efficient approach for benzene-fused 6/7-membered amides via intramolecular amidation of aryl chlorides catalyzed by a Buchwald-Hartwig second generation Pd catalyst (Xphos Pd G2) has been successfully developed. This catalyst system allows the primary amides which have only modest nucleophilicity to be coupled successfully even with electron rich aryl chlorides in short reaction time. The intramolecular amidation reaction also has good chemoselectivity and excellent functional group compatibility.

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.

Thiazine (or oxazine) derivatives and preparation thereof

Thiazine derivatives of the formula [I]: STR1 wherein R1, R2, R4 and R5 are each hydrogen atom; R3 is hydrogen atom or a halogen atom; X is sulfur atom; R6 is naphthyl, a sulfur-containing monoheterocyclic group or a substituted phenyl; Z1 is two hydrogen atoms; Z2 is oxygen atom; A is a lower alkylene; R7 and R8 are the same or different and are each i) hydrogen atom, ii) a lower alkyl, iii) a lower alkenyl, iv) a lower alkynyl, or v) a lower alkyl which is substituted by a substituted phenyl, or both form together with the adjacent nitrogen atom a nitrogen-containing monoheterocyclic group; except for the compound [I] wherein R1, R2, R3, R4 and R5 are each hydrogen atom, X is sulfur atom, R6 is a halogenophenyl, Z1 is two hydrogen atoms, Z2 is oxygen atom, A is a lower alkylene, R7 and R8 are the same or different and each a lower alkyl; or a pharmaceutically acceptable salt thereof, which have calcium antagonistic activity within the cerebral tissues and are useful for prophylaxis and treatment of ischemic encephalopathia.

Naphtho thiazine (or oxaline) derivatives and preparations thereof

Thiazine (or oxazine) derivatives of the formula [I]: STR1 wherein R1 and R2 are both H or form a naphthalene ring together with the benzene ring; R3 and R4 are both H, or one of them is halogen and another is H; X is S or O; R5 and R6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z1 and Z2 is O and another is H2 ; A is lower alkylene; R7 and R8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R1 and R2 are H, Z2 is O and either one of R5 and R6 is substituted phenyl, naphthyl or S-containing heterocyclic group, or their salts, which have calcium antagonistic activity within the cerebral tissues and are useful for prophylaxis and treatment of ischemic encephalopathia and/or cerebral neurocyte dyscrasia, and process for preparing said compounds.