Detail of "119831-72-0"

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Preparation of protected peptide amides using the Fmoc chemical protocol

Preparation of protected peptide amides using the Fmoc chemical protocol. Comparison of resins for solid phase synthesis. Story, Sandra C.; Aldrich, Jane V. (Coll. Pharm., Oregon State Univ., Corvallis, OR, USA). Int. J. Pept. Protein Res., 39(1), 87-92 (English) 1992.In this article, certain chemicals are used. Some of their cas registry numbers are 119831-72-0 and 140848-28-8 CODEN: IJPPC3. ISSN: 0367-8377. DOCUMENT TYPE: Journal CA Section: 34 (Amino Acids, Peptides, and Proteins) Different resins were examd. for their potential use in the solid phase synthesis of protected peptide amides using the 9-fluoroenylmethoxycarbonyl (Fmoc) chem. protocol. The model protected peptide amide Boc-Tyr-Gly-Gly-Phe-Leu-Arg(Pmc)-NH2 (I; Boc = Me3CO2C) was synthesized on both the acid-labile 4-(2',4'-dimethoxyphenyl-Fmoc-aminomethyl)phenoxy resin (Rink amide resin) and on resins contg. the base-labile linker 4-hydroxymethylbenzoic acid. Of the resins examd., only the methylbenzhydrylamine resin contained the 4-hydroxymethylbenzoic acid linkage, which was cleaved by ammonolysis in isopropanol, gave the model peptide I in good overall yield (53% including functionalization). Thus, the synthesis of protected peptide amides by solid phase synthesis using Fmoc-protected amino acids with tert-butyl-type side chain protecting groups is feasible. The choice of peptide-resin linkage and its cleavage conditions, however, are crit. to the success of such syntheses. The potential application of this synthetic strategy to the prepn. of novel peptide amides is discussed. .

Preparation of 1H-4(5)-substituted imidazole derivatives as histamine H3 receptor antagonists

Preparation of 1H-4(5)-substituted imidazole derivatives as histamine H3 receptor antagonists. Phillips, James G.; Tedford, Clark E.; Chaturvedi, Nishith C. (Gliatech, Inc.; Phillips, James G.; Tedford, Clark E.; Chaturvedi, Nishith C., USA). PCT Int. Appl. WO 9638142 A1 5 Dec 1996, 67 pp. DESIGNATED STATES: W: AU, BR, CA, CN, CZ, EE, FI, HU, JP, KR, MX, NZ, PL, TR, UA, US, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM; RW: AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K031-415. ICS: C07D233-60. APPLICATION: WO 1996-US7873 29 May 1996. PRIORITY: US 1995-454522 30 May 1995. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 1, 28, 63 Substituted imidazoles 4-C3H3N2CHR3CHR2XCHR(CH2)nR1 [4-C3H3N2 = 4-imidazolyl, X = NHCO, NMeCO, NHCH2, NMeCH2, CH:CH, COCH2, CH2CH2, CH(OH)CH2, CYC; R = H, Me, NH2, NHMe, NMe2, OH, OMe, SH; n = 0-6, R1 = cycloalkyl, Ph or substituted Ph, heterocyclyl, decahydronaphthyl, octahydroindenyl; R and R1 taken together may form and 5.6 or 6.There are some commonly used reagents with their cas registry numbers 119831-72-0 and 186095-99-8 in this article.6 satd. bicyclic ring when R is NH, O, or S; R2, R3 = H, Me, Et] or their salts were prepd. as histamine H3 receptor antagonists. Thus, phenylalanine-histamine amide was prepd. by coupling Boc-protected phenylalanine with histamine dihydrochloride in THF in the presence of N-methylmorpholine and iso-Bu chloroformate and deprotection using TFA. The histamine H3 receptor binding affinity of the product amide was detd. to be 104 ± 14 nM in rat cortical membranes. .