218163-83-8

Basic information

• Product Name: (1-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester
• Synonyms: (1-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester
• CAS NO: 218163-83-8
• Molecular Weight: 710.701
• Mol File: 218163-83-8.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: (1-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: (1-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester(218163-83-8)
• EPA Substance Registry System: (1-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethylcarbamoyl}-1-methyl-ethyl)-carbamic acid tert-butyl ester(218163-83-8)

Safety Data

• Hazardous Substances Data: 218163-83-8(Hazardous Substances Data)

Upstream product

• 218163-76-9 3a-Pyridin-2-yl-methyl-2-(2,2,2-trifluoroethyl)-2,3a,4,5,6,7-hexahydro-pyrazolo[4,3-c]pyridin-3-one 
• 218163-82-7 Boc-Aib-(D)-O-2,4-diF-Bn-Ser-OH 
• 4377-33-7 2-chloromethylpyridine 
• 218163-74-7 3-Oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester 
• 218163-79-2 N-tert-butoxycarbonylamino-O-(2,4-difluorobenzyl)-D-serine 
• 193274-28-1 4-Oxo-3-(R,S)-pyridin-2-ylmethyl-piperidine-1,3-dicarboxylic Acid 1-tert-butyl ester 3-methyl ester 
• 218163-80-5 (R)-2-Amino-3-(2,4-difluoro-benzyloxy)-propionic acid 
• 161491-24-3 methyl 1-tert-butoxycarbonyl-4-oxo-3-piperidinecarboxylate 
• 108554-34-3 methyl 4-oxonipecotate 
• 23915-07-3 1-(bromomethyl)-2,4-difluorobenzene 

Relevant articles and documents

Discovery and biological characterization of capromorelin analogues with extended half-lives

New tert-butyl, picolyl and fluorinated analogues of capromorelin (3), a short-acting growth hormone secretagogue (GHS), were prepared as part of a program to identify long-acting GHSs that increase 24-h plasma IGF-1 levels. Compounds 4c and 4d (ACD LogD values ≥2.9) displayed extended plasma elimination half-lives in dogs, primarily due to high volumes of distribution, but showed weak GH secretagogue activities in rats (ED50s>10 mg/kg). A less lipophilic derivative 4 (ACD LogD=1.6) exhibited a shorter canine half-life, but stimulated GH secretion in two animal species. Repeat oral dosing of 4 in dogs for 29 days (6 mg/kg) resulted in a significant down-regulation of the post dose GH response and a 60 and 40% increase in IGF-1 levels relative to pre-dose levels at the 8- and 24-h post dose time points. Compound 4 (CP-464709-18) has been selected as a development candidate for the treatment of frailty.