1537906-49-2Relevant academic research and scientific papers
COMPOUNDS OF PHOSPHINANES AND AZAPHOSPHINANES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0314; 0458; 0459, (2018/02/27)
Compounds of formula (I) wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, —N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
Selective alkylation and arylation of C-F bond with grignard reagents
Lu, Faguan,Sun, Hongjian,Du, Aiqin,Feng, Lei,Li, Xiaoyan
, p. 772 - 775 (2014/03/21)
Selective alkylation and arylation of the C-F bonds of polyfluoroaryl imines with Grignard reagents were discovered in the absence of metal catalysts. The aldazine-N atom as an anchoring group has a special effect on the regioselectivity of the reaction. The Ci - N bond addition reaction with Grignard reagents was also explored. A possible mechanism was proposed on the competition between the nucleophilic substitution and addition reaction.
