发明名称 |
Process for the preparation of substituted derivatives of N-ethylglycine |
摘要 |
<p>Prepn. of N-ethyl-glycine derivs. of formula PG-X-CH2CH2-N(CO-B)-CH2COOH (I) or their salts, comprises: (a) reacting protected amino acid derivs. of formula RX-CH2CH2-NH-CH2COOR1 (II) with nucleo-base-acetic acid deriv. of formula B-CH2COOH (III) at 0-45 degrees C in a suitable solvent, and in the presence of a standard peptide coupling agent to give a cpd. of formula RX-CH2CH2-N(COCH2B)CH2COOR1 (IV); (b) removing the acid-labile ester protecting gp. from (IV) (where X = NH the protecting gp. R is also removed) under acid conditions in soln., opt. with addn. of a cation scavenger to give a cpd. of formula HX-CH2CH2N(COCH2B)CH2COOH (V) (when X = O, (IV) may also be treated with a base in an aq. medium); (c) reacting (V) with the appropriate reagent in soln. and in the presence of a base to give (I), and opt. converting to its salt. PG = amino protecting gp. labile in the presence of a weak acid of the urethane or trityl types; X = NH or O; B = standard nucleotide base in which exocyclic amino and OH gps. are protected conventionally; R = H or if X = NH, an acid-labile protecting gp.; and R1 = protecting gp. labile towards acid but stable towards amine. Also new are the intermediates (IV).</p> |
申请公布号 |
EP0761681(A3) |
申请公布日期 |
1997.07.09 |
申请号 |
EP19960113530 |
申请日期 |
1996.08.22 |
申请人 |
HOECHST AKTIENGESELLSCHAFT |
发明人 |
BREIPOHL, GERHARD, DR.;UHLMANN, EUGEN, DR.;WILL, DAVID WILLIAM, DR. |
分类号 |
C07D473/00;C07C231/02;C07C237/22;C07K5/078;C07K14/00;(IPC1-7):C07K5/06 |
主分类号 |
C07D473/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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