Detail of "1585-16-6"

Reference

Preparation of 2-(1H-indol-3-yl)-2-oxo-acetic acid amides with antitumor activity

Preparation of 2-(1H-indol-3-yl)-2-oxo-acetic acid amides with antitumor activity. Menta, Ernesto; Pescalli, Nicoletta (Novuspharma S.p.A., Italy). PCT Int. Appl. WO 2002008225 A1 31 Jan 2002, 35 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, 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, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM; 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: C07D417-12. ICS: A61K031-433; C07D403-12; C07D413-12; A61P035-00. APPLICATION: WO 2001-EP8075 12 Jul 2001. PRIORITY: IT 2000-MI1697 25 Jul 2000. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 The title compds. [I; HET = (un)substituted 4-7 membered (non)arom. heterocyclyl; R3 = H, alkyl, aralkyl, (un)substituted Ph; R4 = alkyl, cycloalkyl, (hetero)aralkyl; X = H, alkyl, OH, etc.] having antitumor activity in particular against solid tumors, specifically colon and lung tumors (no data), were prepd. Thus, reacting 2-[1-(4-fluorobenzyl)-1H-indol-3-yl]-2-oxo-acetyl chloride with 2-amino-1,3,4-thiadiazole in the presence of K2CO3 in 1,2-dimethoxyethane afforded I [HET = 1,3,4-thiadiazol-2-yl; R3 = H; R4 = 4-FC6H4CH2; X = H]. Keywords indolyloxoacetamide prepn antitumor colon lung Index Entries Intestine, neoplasm colon, treatment of; prepn. of 2-(1H-indol-3-yl)-2-oxo-acetamides with antitumor activity Antitumor agents prepn. of 2-(1H-indol-3-yl)-2-oxo-acetamides with antitumor activity Lung, neoplasm treatment of; prepn. of 2-(1H-indol-3-yl)-2-oxo-acetamides with antitumor activity 393795-51-2 393795-52-3 393795-53-4 393795-54-5 393795-55-6 393795-56-7 393795-57-8 393795-58-9 393795-59-0 393795-60-3 393795-61-4 96-50-4 111-83-1 120-72-9, reactions 1585-16-6 4005-51-0 85607-00-7 204205-77-6 393795-63-6 42951-63-3 348111-46-6 348111-47-7 348111-48-8 348111-50-2 348111-64-8 393795-62-5 prepn. of 2-(1H-indol-3-yl)-2-oxo-acetamides with antitumor activity

Synthesis of m-(aminomethyl)benzoic acid peptides

Synthesis of m-(aminomethyl)benzoic acid peptides. Stewart, Frederick H. C. (Div. Protein Chem., CSIRO, Parkville 3052, Australia). Aust. J.There are some reagents with their cas registry numbers 1585-16-6 and 89760-76-9 are used in this study. Chem., 36(12), 2511-16 (English) 1983. CODEN: AJCHAS. ISSN: 0004-9425. DOCUMENT TYPE: Journal CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 25 Title peptides H-Gly-Gly-Amb-OH [I, Amb = m-(H2NCH2)C6H4CO], H-Amb-Amb-OH (II), and H-Gly-Amb-Gly-OH were prepd. by conventional soln. methods. Thus, Z-Gly-Gly-ONp (Z = PhCH2O2C, Np = C6H4NO2-p) was coupled with H-Amb-OTmb.HCl (Tmb = CH2C6H2Me3-2,4,6) in DMF contg. Et3N to give 99% Z-Gly-Gly-Amb-OTmb, which was deblocked by HBr/HOAc to give 79% I. Z-Amb-ONp was coupled with H-Amb-OTmb to give 89% Z-Amb-Amb-OTmb, which was deblocked to give 87% II. Z-Tyr(CH2Ph)-ONSu (NSu = succinimido) was coupled with H-Amb-OH to give Z-Tyr(CH2Ph)-Amb-OH, which was used in the conventional synthesis of enkephalin analog H-Tyr-Amb-Phe-Leu-OH. .