192315-37-0

Upstream product

• 782440-99-7 3-chloro-L-tyrosine methyl ester 
• 232277-27-9 methyl (S)-3-(3-chloro-4-hydroxyphenyl)-2-((tert-butoxycarbonyl)amino) propanoate 
• 74-88-4 methyl iodide 
• 3417-91-2 L-tyrosine methyl ester HCl 
• 60-18-4 L-tyrosine 
• 121056-95-9 trimethyl 2-(tert-butoxycarbonylamino)phosphonoacetate 
• 4903-09-7 3-chloro-4-methoxy-benzaldehyde 
• 1270191-76-8 (Z)-methyl 3-(3-chloro-4-methoxyphenyl)-2-(tert-butoxycarbonylamino)acrylate 

Relevant academic research and scientific papers

Synthesis and trypanocide activity of chloro-l-tyrosine and bromo-l-tyrosine derivatives

Twenty-two halogenated l-tyrosine derivatives were synthesized to examine new substances for the treatment of Chagas disease. The synthesis of these derivatives with different degree of substitution in the amino group with methyl iodide, giving primary, tertiary, and quaternary amino acids. All compounds were tested in vitro against intracellular amastigotes of Trypanosoma cruzi, and the cytotoxicity were evaluated over monocytic cell line U-937. Compound 25 was the most active against T. cruzi with a EC50 of 75.52 μM compared with benznidazole with a EC50 of 58.79 μM. Compounds 3, 4, 7, and 15 were the derivatives with the best selectivity index (SI) with values of 7.5, 8.3,12.1, and 8.6, respectively. Finally, compound 7 was the safer and the more promising derivative against T. cruzi.

A two step synthesis of a key unit B precursor of cryptophycins by asymmetric hydrogenation

A novel highly enantioselective two step access to a unit B precursor of cryptophycins in good yields from commercially available starting materials has been developed. The key step is an asymmetric hydrogenation using the commercially available [(COD)Rh-