- Preparation and structure confirmation new methods of (S)-3-Boc-aminomethylpiperidine
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The invention discloses preparation and structure confirmation of (S)-3-Boc-aminomethylpiperidine. A compound 5 is obtained by benzylation of a compound 1, reduction of a carbonyl group, protection ofan amino group, and catalytic hydrogenation; then the compound 5 is subjected to derivation to obtain a crystal; the crystal is subjected to diffraction test and analyzed to obtain that the compound5 is the (S)-3-Boc-aminomethylpiperidine, and the optical rotation is -8.98, which further proves that the method for preparing the compound 5 is feasible. According to the preparation method, the cheap and easily available chiral raw material compound 1 is used without using a resolving agent, and the advantages in yield and cost are realized; the product is tested by derivatization and diffraction way to determine the correct configuration, and the preparation and confirmation methods form a system, thereby facilitating industrial production and realizing a broad application prospect.
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Paragraph 0025; 0029; 0037; 0038; 0058
(2018/09/11)
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- CHIRAL 1-(4-METHYLPHENYLMETHYL)-5-OXO-{N-[(3-T-BUTOXYCARBONYL- AMINOMETHYL)]-PIPERIDIN-1-YL}-PYRROLIDINE-2-CARBOXAMIDES AS INHIBITORS OF COLLAGEN INDUCED PLATELET ACTIVATION AND ADHESION
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Chiral l-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]- piperidin-l-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion The present invention provides chiral (2S)-l-(4-methylphenylmethyl)-5-oxo-(3S)-{N-[(3-t- butoxycarbonyl aminomethyl)]-piperidin-l-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4- methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-l-yl}- pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p- methylphenylmethyl)lpyroglutamate in good chiral purity.
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Page/Page column 17-18
(2012/08/27)
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