Reference

Process for the preparation of benzylamine derivative containing spiro[isoquinoline-1,4'-piperidine] moiety

All Rights Reserved. Process for the preparation of benzylamine derivative containing spiro[isoquinoline-1,4'-piperidine] moiety. Nagasawa, Masaaki; Murata, Masakazu; Kawase, Nobuo; Nakao, Ryu; Nakano, Daisuke (Zeria Pharmaceutical Co., Ltd., Japan). PCT Int. Appl. WO 2007007846 A1 18 Jan 2007, 47pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (Japanese). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-JP313997 13 Jul 2006. PRIORITY: JP 2005-205323 14 Jul 2005. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1 Process for producing compds. I [R1 = alkyl, aryl, aralkyl; R2 = (un)substituted alkyl; R3 = alkyl, (un)substituted aryl or aralkyl; R4 = alkyl, aryl, aralkyl, etc.; X1, X2 = H, halo], characterized by reaction of compd. II [R1-R4, X1, X2 = same as above] with 2H-spiro[isoquinoline-1,4'-piperidine]-3(4H)-one, was disclosed. For example, to a soln. of (S)-N-[2-(3,4-dichlorophenyl)-1-(3,3,3-trifluoro-N-methylpropanamido)p ent-4-en-2-yl]-N-methylbenzamide (58.8 kg) in acetonitrile (200 L) was added NaIO4 (45.2 kg)/water (520 L)/acetonitrile (730 L). Treatment of the resulting mixt. with RuCl3 hydrate (983 g) at ￡5° for 1 h afforded a mixt. of compd. III [R = CHO] and N-[2-(3,4-dichlorophenyl)-4,5-dihydroxy-1-(3,3,3-trifluoro-N-methylpropa namido)pentan-2-yl]-N-methylbenzamide (IV) in 85.6% purity. The mixt. of III [R = CHO] and IV in acetonitrile (200 L) was exposed to NaIO4 (51.6 kg)/water (400 L) to give compd. III [R = CHO] in 84.4% purity. To the obtained compd. 2516-99-6 and 919534-39-7 which are cas registry numbers of substances are two of reagents here. III [R = CHO] in Et acetate (200 L) was added a soln. of 2H-spiro[isoquinoline-1,4'-piperidine]-3(4H)-one (26.1 kg), sodium acetoxyborohydride (27.0 kg) and acetic acid in THF (140 L) at ￡10°, then the reaction was stirred for 3 h to afford compd. III [R = Q] (83.2 kg), which is useful as a tachykinin receptor antagonist. .

Suicide inactivation of enzymes

Suicide inactivation of enzymes. Generalities and application to fructose 1,6-diphosphate aldolase.Several substances are used for example 2516-99-6 which is its cas registry number. Le Clef, B.; Magnien, A.; Biellmann, J. F. (Inst. Chim., Univ. Louis Pasteur, Strasbourg F 67008, Fr.). Ann. Chim. (Paris), 9(6), 703-8 (English) 1984. CODEN: ANCPAC. 2516-99-6 is just another one chemical used in this study. ISSN: 0151-9107. DOCUMENT TYPE: Journal CA Section: 7 (Enzymes) 1-Hydroxy 2-keto 4,4,4-trifluorobutane phosphoric acid (HFTP) was prepd. from 3,3,3-trifluoropropionic acid. HFTP acts as an irreversible inhibitor of rabbit muscle fructose 1,6-diphosphate aldolase. ..