Reference

Preparation of b,b-dialkyl analogs of cysteine suitable for peptide synthesis

Preparation of b,b-dialkyl analogs of cysteine suitable for peptide synthesis. Stanfield, C.Several substances are used for example 24424-99-5 and 96-22-0 which are their cas registry numbers. Freeman; Cody, Wayne L.; Hruby, Victor J. (Dep. Chem., Univ. Arizona, Tucson, AZ 85721, USA). J. Org. Chem., 51(26), 5153-6 (English) 1986. CODEN: JOCEAH. ISSN: 0022-3263. DOCUMENT TYPE: Journal CA Section: 34 (Amino Acids, Peptides, and Proteins) The synthesis of title cysteine analogs HSCRR1CH(NH2)CO2H.HCl [I; R = R1 = Et; RR1 = (CH2)4, (CH2)5, CH2CH2CH(CMe3)CH2CH2] was based on the sulfenylation of dehydroamino acids II. Thus, CNCH2CO2Et were condensed with ketones RR1CO (R, R1 = same) to give the corresponding II, which underwent sulfenylation with P4S10 in refluxing benzene to give thiazolines III, which were hydrolyzed by aq. HCl to give I. The SH groups of I were protected with p-MeC6H4CH2Cl in liq. NH3 contg. Na to give cysteines IV (R2 = H), which were N-protected with (Boc)2O to give IV (R2 = Boc). The latter protected derivs. are suitable for soln. or solid-phase peptide coupling. .

Design and synthesis of orally active benzamide derivatives as potent serotonin 4 receptor agonist

Design and synthesis of orally active benzamide derivatives as potent serotonin 4 receptor agonist.Several substances are used for example 24424-99-5 and 188971-45-1 which are their cas registry numbers. Sonda, Shuji; Kawahara, Toshio; Murozono, Takahiro; Sato, Noriko; Asano, Kiyoshi; Haga, Keiichiro (Pharmaceutical Development Laboratories, Technology & Production Division, Mitsubishi Pharma Corporation, Yoshitomi-cho, Chikujo-gun Fukuoka 871-8550, Japan). Bioorganic & Medicinal Chemistry, 11(19), 4225-4234 (English) 2003 Elsevier Science Ltd. CODEN: BMECEP. ISSN: 0968-0896. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27 A series of 4-amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamide derivs. bearing an aralkylamino, alkylamino, benzoyl or phenylsulfonyl group at its side chain part at the 1-position on the piperidine ring was synthesized. They were evaluated for serotonin 4 (5-HT4) receptor agonist activity by testing their ability to contract the isolated guinea-pig ascending colon. 4-Amino-5-chloro-2-methoxy-N-[1-[5-(1-methylindol-3-ylcarbonylamino) pentyl]piperidin-4-ylmethyl]benzamide (1a, Y-34959) and its related compds. possessed favorable pharmacol. profiles for gastrointestinal motility. Unfortunately, the compd. 1a showed low bioavailability when given orally presumably due to its poor intestinal absorption rate. Replacement of the 1-methylindol-3-yl carbonylamino moiety of 1a with an aralkylamino (or alkylamino) group did not improve the intestinal absorption rate. Replacement of the 1-methylindol-3-ylcarbonylamino moiety with a benzoyl or phenylsulfonyl group increased the intestinal absorption rate compared with 1a. These compds. revealed good pharmacol. profiles for gastrointestinal motility and were superior to 1a in oral bioavailability. .