Reference

Method for producing an optically active b-amino acid

Method for producing an optically active b-amino acid. Matsumura, Kazuhiko; Zhang, Xiaoyong; Saito, Takao (Takasago International Corporation, Japan). Eur. Pat. Appl. EP 1386901 A1 4 Feb 2004, 22 pp. DESIGNATED STATES: R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE, MC, PT, IE, SI, LT, LV, FI, RO, MK, CY, AL, TR, BG, CZ, EE, HU, SK. (English). (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07B053-00. ICS: C07C227-32; C07C229-08. APPLICATION: EP 2003-16551 24 Jul 2003. PRIORITY: JP 2002-222149 30 Jul 2002. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) Optically active b-amino acids H2NCHR1CHR2COR3 [R1 is H, (un)substituted alkyl, cycloalkyl, aralkyl, aryl, heterocyclyl, alkoxy, aralkoxy, or aryloxy; R2 is any group given for R1 or (un)substituted alkoxycarbonyl; R3 is (un)substituted alkoxy, aralkoxy, aryoxy, or amino] and their salts, useful as intermediates for the prodn. of medicines, agricultural chems. 10472-24-9 and 288254-55-7 which are cas registry numbers of chemicals are mentioned. and physiol. active substances, were prepd. by asym. hydrogenation of enamines H2NCR1:CR2COR3 or their salts. Thus, Me 3-amino-3-phenylacrylate in MeOH was hydrogenated over Ru(OAc)2[(R)-H8-binap] in the presence of chloroacetic acid at 50° and 3 MPa H2 pressure for 88 h to afford 39.5% Me (S)- 3-amino-3-phenylpropionate. .

Stable peptide derivatives for the preparation of radiopharmaceuticals

Stable peptide derivatives for the preparation of radiopharmaceuticals. Sworin, Michael; Rajopadhye, Milind; Harris, Thomas David; Edwards, David Scott; Cheesman, Edward Hollister; Liu, Shuang (Du Pont Merck Pharmaceutical Company, USA). PCT Int. Appl. WO 9640637 A1 19 Dec 1996, 114 pp. DESIGNATED STATES: W: AM, AT, AU, AZ, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, HU, IL, JP, KG, KR, KZ, LT, LU, LV, MD, MX, NO, NZ, PL, PT, RO, RU, SE, SG, SI, SK, TJ, TM, UA, VN, 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: C07D213-82. ICS: C07D401-12; C07D401-14; A61K051-04; A61K031-44. APPLICATION: WO 1996-US9766 7 Jun 1996.In this article, certain chemicals are used. Some of their cas registry numbers are 186304-74-5 and 10472-24-9 PRIORITY: US 1995-476296 7 Jun 1995. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 1, 63 Novel reagents for the prepn. of radiopharmaceuticals comprise a biol. active group connected to a stable hydrazone group, optionally via a linking group. The biol. active mol. is selected from IIb/IIIa receptor antagonists, IIb/IIIa receptor ligands, fibrin binding peptides, leukocyte binding peptides, chemotactic peptides, somatostatin analogs, and selectin binding peptides. The reagents react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of diseases and thus allow an image to be obtained of the loci using gamma scintigraphy. Thus, the benzaldehyde hydrazone of cyclo[D-Val-NMeArg-Gly-Asp-Mamb(hydrazinonicotinyl-5-Aca)] (Mamb = 3-aminomethylbenzoic acid, Aca = aminocaproamide) was prepd. by reaction of cyclo[D-Val-NMeArg-Gly-Mamb(5-Aca)].2TFA with succinimidyl 6-(2-benzaldehydehydrazino)nicotinate in DMF at room temp. for 42 h. The product was converted into the 99mTc-based radiopharmaceutical. .