1215074-48-8

Basic information

• Product Name: TERT-BUTYL 4-AMINO-2-METHOXYBENZOATE
• Synonyms: TERT-BUTYL 4-AMINO-2-METHOXYBENZOATE
• CAS NO: 1215074-48-8
• Molecular Formula: C₁₂H₁₇NO₃
• Molecular Weight: 223.26828
• Mol File: 1215074-48-8.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• CAS DataBase Reference: TERT-BUTYL 4-AMINO-2-METHOXYBENZOATE(CAS DataBase Reference)
• NIST Chemistry Reference: TERT-BUTYL 4-AMINO-2-METHOXYBENZOATE(1215074-48-8)
• EPA Substance Registry System: TERT-BUTYL 4-AMINO-2-METHOXYBENZOATE(1215074-48-8)

Safety Data

• Hazardous Substances Data: 1215074-48-8(Hazardous Substances Data)

Upstream product

• 2597-56-0 4-nitro-o-anisic acid 
• 1232688-45-7 tert-butyl 2-methoxy-4-nitrobenzoate 

Downstream Products

• 1272527-36-2 4-(3,5-dichloro-4-ethoxybenzamido)-2-hydroxybenzoic acid 
• 1272528-44-5 tert-butyl 4-(3,5-dichloro-4-ethoxybenzamido)-2-methoxybenzoate 

Relevant articles and documents

Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist

A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5, which has good selectivity over the RARβ and RARγ receptors. Analysis of the medicinal chemistry parameters of the 3,5-substituents of derivatives of template 5 enabled us to design a class of drug-like molecules with lower intrinsic clearance and higher oral bioavailability which led to the novel RARα agonist 4-(3-chloro-4-ethoxy-5-isopropoxybenzamido)-2-methylbenzoic acid 56 that has high RARα potency and excellent selectivity versus RARβ (2 orders of magnitude) and RARγ (4 orders of magnitude) at both the human and mouse RAR receptors with improved drug-like properties. This RARα specific agonist 56 has high oral bioavailability (>80%) in both mice and dogs with a good PK profile and was shown to be inactive in cytotoxicity and genotoxicity screens.

AMIDE DERIVATIVE

The present invention relates to a compound or a pharmacologically acceptable salt thereof that has an excellent antagonistic effect on a neurokinin NK1 receptor, a neurokinin NK2 receptor, and a muscarine M3 receptor and is useful as a therapeutic agent for bronchial asthma, chronic obstructive pulmonary disease, or the like. A compound represented by general formula (I): [wherein R1 represents a hydrogen atom, a C1-C6 alkyl group, or the like; R2 represents a hydrogen atom, a C1-C6 alkyl group, or the like; R3 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group A, or the like; R4 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group A, or the like; L1 represents a C1-C10 alkylene group or the like; L2 represents a carbonyl group, a group represneted by the formula -N(R5)-C(=O)-, a group represented by the formula -C(=O)-N(R5)-, or the like; R5 represents a hydrogen atom, a C1-C6 alkyl group, or the like; E represents a phenylene group that may be substituted with 1 to 4 group(s) independently selected from Substituent Group A, or the like; m is an integer of 1 to 4; n is an integer of 0 to 4; p is an integer of 0 to 2; q is an integer of 1 to 10; r is 1 or 2; s is 0 or 1; and Substituent Group A represents the group consisting of a halogen atom, a C1-C6 alkyl group, C1-C6 halogenated alkyl group, or the like] or a pharmacologically acceptable salt thereof.

DIHYDROPYRIDONE UREAS AS P2X7 MODULATORS

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.