Detail of "2045-79-6"

Reference

Process for preparation of novel amino acid amide derivative

Process for preparation of novel amino acid amide derivative. Rew, Yo Sup; Kim, Sung Kee; Lee, Yeo Ho; Yu, Sung Hoon; Jeon, Jae Hoon; Pyun, Seun Yup; Choi, Woo Bong; Chun, Sung Wook; Chun, Sam Jae; Lee, Seong Baek; Park, Hyun Cheol; Kim, Mun Jung; Cho, Jin Ho (LG Chemical Co., Ltd, S. Korea). Repub. Korea KR 201583 B1 15 Jun 1999, No pp. given (Korean). (Korea, Republic Of). CODEN: KRXXFC. CLASS: ICM: C07C237-08. APPLICATION: KR 1997-7131 4 Mar 1997. PRIORITY: KR 1996-5863 6 Mar 1996. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 1 Provided is a method for manufg. a novel amino acid amide deriv. which is useful as a sterilizing agent in preventing proliferation of Oomycetes and Botrytis.Several substances like 2045-79-6 may be metioned in this study. A novel amino acid amide deriv. is manufd. by the following steps of: (i) reacting 2-methoxy-2-phenyl-ethylamine compd. with a compd. of the formula (III), in the presence of solvent and base, at minus 30-70°, preferably at 10-30°, for 10 min to 24 h; (ii) hydrolyzing a compd. of the formula (I-1) with a large amt. of trifluoroacetic acid at 10-30° for 30 min to 5 h; and (iii) reacting a compd. of the formula (I-2) with a compd. of the formula (IV), in the presence of base and solvent, at minus 10-40° for 10 min-24 h. In the formula (I), each X1 and X2 is hydrogen, or methoxy, Me, or halogen group; when X1 and X2 are bound with the carbon atom of a benzene ring, they can form a methylenedioxy group; R1 is hydrogen, Ph group, or -CHR5R6 (wherein, R4 is cyclopropyl, chloroethyl, alkyl of C1-C4; alkoxy of C1-C4; haloalkoxy of C1-C3, aryloxy, or benzyloxy); R2 is hydrogen; and R3 is hydrogen. .

Preparation of 3,9-diazabicyclo[3

Preparation of 3,9-diazabicyclo[3.3.1]nonene derivatives as inhibitors of parasite aspartic proteases. Bur, Daniel; Fischli, Walter; Remen, Lubos; Richard-Bildstein, Sylvia; Weller, Thomas; Boss, Christoph; Binkert, Christoph; Meyer, Solange ( Actelion Pharmaceuticals Ltd., Switz.). PCT Int. Appl. WO 2004105762 A1 9 Dec 2004, 177 pp. 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, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K031-4995. ICS: A61P033-06. APPLICATION: WO 2004-EP5065 12 May 2004. PRIORITY: WO 2003-EP5661 30 May 2003. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 7 Pharmaceutical compns. for treating diseases demanding the inhibition of parasite aspartic proteases contain one or more compd.(s) of the general formula (I) [X, W = N, CH; V = (CH2)r, A-(CH2)s, CH2-A-(CH2)t, (CH2)s-A, (CH2)2-A-(CH2)u-; A(CH2)v-B, (CH2)3-A-CH2, A-CH2CH2-B-CH2, CH2-A-CH2CH2-B, (CH2)3-A-CH2CH2, (CH2)4-A-CH2, A-CH2CH2-B-CH2-CH2, CH2-A-CH2-CH2-B-CH2, CH2-A-(CH2)3-B, CH2CH2-A-CH2CH2-B (wherein A, B = O, S, SO, SO2; r = 3-6; s = 2-5; t = 1-4; u = 1-3; v = 2-4); U = aryl, heteroaryl; T = CONR1, (CH2)pOCO, (CH2)pN(R1)CO, (CH2)pN(R1)SO2, COO (wherein R1 = H, lower alkyl, alkenyl, or alkynyl, etc.; p = 1-4); Q = lower alkylene or alkenylene; M = H, cycloalkyl, aryl, heterocyclyl, heteroaryl; L = R3, COR3, COOR3, CONR2R3, SO2R3, SO2NR2R3, COCH(Aryl)2 (wherein R2 = H, lower alkyl or alkenyl, cycloalkyl, cycloalkyl-lower alkyl; R3 = H, each (un)substituted lower alkyl or alkenyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, cycloalkyl-lower alkyl, aryl-lower alkyl, heteroaryl-lower alkyl, heterocyclyl-lower alkyl, aryloxy-lower alkyl, or heteroaryloxy-lower alkyl); m, n = 0 or 1], optically pure enantiomers, mixts. of enantiomers such as racemates, diastereomers, mixts. of diastereomers, diastereomeric racemates, mixts. of diastereomeric racemates, and the meso-form as well as pharmaceutically acceptable salts, solvent complexes and morphol. forms and suitable carrier materials. The pharmaceutical compns. are useful for the treatment or prevention of malaria or diseases caused by protozoal infection. The invention also concerns related aspects including processes for the prepn. There are some commonly used reagents like 2045-79-6 in this article. of the pharmaceutical compns. contg. one or more of those compds. and esp. their use as inhibitors of plasmepsin II. For example, compd. (II) showed IC50 of <10 nM against plasmepsin II. .