58483-95-7

Usage

Uses

Used in Pharmaceutical Industry:
5-AMINO-2-CHLOROPYRIDINE-4-CARBOXYLIC ACID is used as a synthetic intermediate for the development of various pharmaceutical compounds. Its application is primarily due to its ability to be used in the preparation of inhibitors targeting the EGFr (Epidermal Growth Factor Receptor) and c-erbB-2 (Human Epidermal Growth Factor Receptor 2), which are significant in the treatment of certain types of cancer.
Additionally, 5-AMINO-2-CHLOROPYRIDINE-4-CARBOXYLIC ACID is utilized in the synthesis of modulators of GHSr-1a, which are crucial for the treatment of type II diabetes and obesity. These modulators help regulate the growth hormone secretion and improve the overall metabolic profile in patients.

InChI:InChI=1/C6H5ClN2O2/c7-5-1-3(6(10)11)4(8)2-9-5/h1-2H,8H2,(H,10,11)

Upstream product

• 1072-98-6 5-chloro-2-pyridylamine 
• 5350-93-6 6-Chloro-pyridin-3-ylamine 
• 171178-45-3 tert-butyl (6-chloropyridin-3-yl)carbamate 
• 5326-23-8 6-Chloro-3-pyridinecarboxylic acid 
• 171178-46-4 5-[N-(tert-butoxycarbonyl)amino]-2-chloropyridine-4-carboxylic acid 

Downstream Products

• 171178-47-5 6-chloro-3H-pyrido[3,4-d]pyrimidin-4-one 
• 171178-48-6 4,6-dichloro-pyrido<3,4-d>pyrimidine 
• 189680-99-7 4-chloro-6-(N,N-dimethylamino)-pyrido[3,4-d]pyrimidine 
• 189680-98-6 6-dimethylamino-3H-pyrido[3,4-d]pyrimidin-4-one 
• 202272-67-1 (1-benzyl-1H-indazol-5-yl)-(6-chloropyrido[3,4-d]pyrimidin-4-yl)-amine 
• 202272-97-7 (1-Benzyl-1H-indol-5-yl)-(6-chloro-pyrido[3,4-d]pyrimidin-4-yl)-amine 
• 202272-68-2 GW2974 
• 202272-71-7 (2-benzyl-1H-benzimidazol-5-yl)-(6-chloro-pyrido[3,4-d]pyrimidin-4-yl)-amine 
• 1073182-59-8 methyl 5-amino-2-chloroisonicotinate 
• 1594729-07-3 6-(3-fluorophenyl)pyrido[3,4-d]pyrimidin-4-amine 
• 183741-98-2 6-methoxypyrido[3,4-d]pyrimidin-4(3H)-one 
• 1073182-66-7 3-amino-6-chloro-2-methylisonicotinic acid 
• 1073182-63-4 3-amino-6-chloro-2-methylisonicotinic acid methyl ester 

Relevant academic research and scientific papers

Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR

The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.

HETEROCYCLIC HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME

A hydrazide compound represented by the formula (I), an N-oxide thereof or suitable salt thereof: has excellent pesticidal activity.

QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS

The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

PYRIDO [3,4-D] PYRIMIDINE DERIVATIVES AS MATRIX METALLOPROTEINASE-13 INHIBITORS

This invention relates to a pyrido[3,4-d]pyrimidine derivative of Formula (I), or a pharmaceutically acceptable salt thereof, wherein R, L', L2, V, L3, and R2 are as defined in the specification, that inhibits a matrix metalloproteinase-13 enzyme and thus is useful for treating diseases resulting from MMP-13 mediated tissue breakdown such as osteoarthritis, rheumatoid arthritis, cartilage damage, psoriatic arthritis, ankylosing spondylitis, heart failure, atherosclerosis, inflammatory bowel disease, multiple sclerosis, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, cancer, and osteoporosis.

Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and c-erbB-2

Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N4-(1-benzyl-1H-indazol-5-yl)-N6,N6- dime

Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives

Directed lithiation of Boc or pivaloyl derivatives of 2-substituted 5-aminopyridines with BuLi-TMEDA in diethyl ether at -10°C gave 4-lithio derivatives which were quenched with CO2 to give the analogous C-4 carboxylic acids. Hydrolysis of the protecting groups with either TFA or aqueous KOH gave 2-substituted 5-aminopyridine-4-carboxylic acids which were converted to 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones by reaction with formamide or, more optimally, formamidine acetate. Boc protected aminopyridines provided the best overall results, with synthesis of these derivatives best achieved by direct reaction of the aminopyridine with di-tert-butyl dicarbonate in the absence of added base.