206268-37-3

Upstream product

• 533-58-4 2-Iodophenol 
• 93267-04-0 N-(tert-butoxycarbonyl)-L-3-iodoalanine methyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 72683-81-9 methyl (2R)-2-amino-3-(2-hydroxyphenyl)propanoate hydrochloride 
• 24008-77-3 (2R)-2-amino-3-(2-hydroxyphenyl)propanoic acid 

Downstream Products

• 183500-01-8 3-(2-hydroxyphenyl)-2-(N-t-butoxycarbonylamino)propanol 
• 1024615-66-4 methyl N-{[(1,1-dimethylethyl)oxy]carbonyl}-3-[(phenylmethyl)oxy]-L-phenylalaninate 
• 1024615-64-2 methyl N-{[(1,1-dimethylethyl)oxy]carbonyl}-2-(phenoxy)-L-phenylalaninate 

Relevant academic research and scientific papers

Much improved conditions for the Negishi cross-coupling of iodoalanine derived zinc reagents with aryl halides

(Chemical Equation Presented) A combination of Pd2(dba) 3 and SPhos (1:2 molar ratio) is an excellent precatalyst for the Negishi cross-coupling of the serine-derived organozinc reagent 2 with aryl halides, including previously difficult ortho-substituted examples. In the case of meta- and para-substituted aryl halides, Pd-loadings of 0.5 mol % give satisfactory results. Use of 2-iodoaniline as substrate gives the lactam 12 in good yield. 2009 American Chemical Society.

2-((5-(PHENYL)-PYRROLO[2,1-F][1,2,4]TRIAZIN-4-YL)AMINO)-3-(PHENYL)PROPANOIC ACID DERIVATIVES AND RELATED COMPOUNDS AS MCL-1 ENZYME INHIBITORS FOR TREATING CANCER

A compound of formula I (the variables are defined in the claims) or a pharmaceutically acceptable salt or solvate thereof, as an MCL-1 enzyme inhibitor for treating colon cancer, breast cancer, small-cell lung cancer, non-small- cell lung cancer, bladder cancer, ovarian cancer, prostate cancer, chronic lymphoid leukemia, lymphoma, myeloma, acute myeloid leukemia, or pancreatic cancer. The present description discloses the synthesis of exemplary compounds as well as biological assays thereof (e.g. pages 55 to 114; paragraphs [00216] to [00304]; examples 1 to 33; tables A and 2). An exemplary compound is e.g. (2R)-2-{[(5Ra)-5-{3-chloro-2-methyl-4-[2-(4-methylpiperazin-l-yl) ethoxy]phenyl}-6-(4-fluorophenyl) py rrolo[2, l-f][l, 2, 4]triazin-4-yl]am ino}-3-(2-{[2-(2-methoxy phenyl) py rim idin-4-yl]methoxy} phenyl) propanoic acid (example 13) with e.g. 0.7 nM BIM_Ki in an cell free MCL-1 Bim affinity assay.

Thiol-based angiotensin-converting enzyme 2 inhibitors: P1′ modifications for the exploration of the S1′ subsite

Explorations of the S1′ subsite of ACE2 via modifications of the P1′ methylene biphenyl moiety of thiol-based metalloprotease inhibitors led to improvements in ACE2 selectivity versus ACE and NEP, while maintaining potent ACE2 inhibi