Detail of "22032-65-1"

Reference

Preparation of pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-diones as cGMP-specific phosphodiesterase inhibitors

Preparation of pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-diones as cGMP-specific phosphodiesterase inhibitors. Daugan, Alain Claude-Marie; Gellibert, Francoise (Laboratoire Glaxo Wellcome S.A.; Daugan, Alain Claude-Marie; Gellibert, Francoise, Fr.). PCT Int. Appl. WO 9703985 A1 6 Feb 1997, 24 pp. DESIGNATED STATES: W: AL, AM, AT, AU, AZ, BB, BG, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, NL, PT, SE. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D471-14. ICS: A61K031-395. ICI: C07D471-14, C07D241-00, C07D221-00, C07D209-00. APPLICATION: WO 1996-EP3025 11 Jul 1996. PRIORITY: GB 1995-14465 14 Jul 1995. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 The title compds.There are some commonly used reagents with their cas registry numbers 22032-65-1 and 187939-83-9 in this article. [I; R0 = H, halo, C1-6 alkyl; R1 = H, C1-6 alkyl; R2 = (un)substituted benzofuranyl; R3 = H, C1-3 alkyl], useful as potent and selective inhibitors of cGMP-specific PDE, were prepd. and formulated. Thus, cyclization of (1R,3R)-Me 1,2,3,4-tetrahydro-1-(5-benzofuranyl)-2-chloroacetyl-9H-pyrido[3,4-b]ind ole-3-carboxylate with MeNH2 in MeOH/EtOH afforded (6R,12aR)-I [R0, R3 = H; R1 = Me; R2 = 5-benzofuranyl] which showed IC50 of 15 nM against cGMP-specific PDE in vitro, and AUC (area under curve of the fall in blood pressure) of 137 mm Hg.h in spontaneously hypertensive rats. .

Recemization of a-amino acid esters

Recemization of a-amino acid esters. Dotani, Masaharu; Igarashi, Hideo; Kondo, Toshio; Uchiyama, Takako (Mitsubishi Gas Chemical Co., Inc., Japan). Jpn. Kokai Tokkyo Koho JP 61251647 A2 8 Nov 1986 Showa, 4 pp. (Japan) CODEN: JKXXAF. CLASS: ICM: C07C101-04. ICS: C07C099-00. ICA: C07B055-00. APPLICATION: JP 85-93237 30 Apr 1985. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) H2HCRCO2R1 [R = H, furyl, pyridyl, thiazolyl, imidazolyl, indolyl, (un)substituted lower alkyl, Ph; R1 = lower alkyl] (optically active) were racemized by treating with alkali metal alcoholates or alkali metal amides without solvents. Thus, 26 g D-valine iso-Bu ester was stirred with 0.32 g NaOMe at 20° for 20 min to give DL-valine iso-Bu ester in 93% racemization. 22032-65-1 and 107998-45-8 are just another two chemicals used in this study. .