Synthesis of (2S,4R,5R)-4,5,6-trihydroxynorleucine and 5-hydroxynorvaline from precursors obtained by an unusual rearrangement in a 5,6-dihydro-2-pyrone

2-Acetamido-4,6-O-benzylidene-2,3-dideoxy-D-erythro-hex-2-enono-1,5-la ctone (2), readily prepared from D-glucosamine, undergoes a rearrangement on treatment with tin(IV) chloride which leads to 3-acetamido-2-pyrone (3) and 2-acetamido-2,3-dideoxy-4,6-O-formylidene-D-threo-hex-2-enono-1,5-lact one (...

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Autor principal: Nin, A.P
Otros Autores: De Lederkremer, R.M, Varela, O.
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: Elsevier Ltd 1996
Acceso en línea:Registro en Scopus
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Registro en la Biblioteca Digital
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030 |a TETRA 
100 1 |a Nin, A.P. 
245 1 0 |a Synthesis of (2S,4R,5R)-4,5,6-trihydroxynorleucine and 5-hydroxynorvaline from precursors obtained by an unusual rearrangement in a 5,6-dihydro-2-pyrone 
260 |b Elsevier Ltd  |c 1996 
270 1 0 |m Varela, O.; Departamento de Quimica Organica, Facultad Ciencias Exactas/Naturales, Universidad de Buenos Aires, Ciudad Universitaria, 1428 Buenos Aires, Argentina 
506 |2 openaire  |e Política editorial 
504 |a Varela, O., Nin, A.P., Lederkremer, R.M., (1994) Tetrahedron Lett., 35, pp. 9359-9362 
504 |a Nin, A.P., Varela, O., Lederkremer, R.M., (1993) Tetrahedron, 49, pp. 9459-9464 
504 |a Wagner, I., Musso, H., (1983) Angew. Chem. Int. Ed. Engl., 22, pp. 816-828 
504 |a Cintas, P., (1991) Tetrahedron, 47, pp. 6079-6111 
504 |a Lederkremer, R.M., Varela, O., (1994) Adv. Carbohydr. Chem. Biochem., 50, pp. 125-209 
504 |a Horton, D., Thomson, J.K., Varela, O., Nin, A.P., Lederkremer, R.M., (1989) Carbohydr. Res., 193, pp. 49-60 
504 |a Nin, A.P., Varela, O., Lederkremer, R.M., (1991) Synthesis, pp. 73-74 
504 |a Garbish E.W., Jr., (1964) J. Am. Chem. Soc., 86, pp. 5561-5564 
504 |a Nelson, C.R., Gratzl, J.S., (1978) Carbohydr. Res., 60, pp. 267-273 
504 |a Evans, M.E., (1972) Carbohydr. Res., 21, pp. 473-475 
520 3 |a 2-Acetamido-4,6-O-benzylidene-2,3-dideoxy-D-erythro-hex-2-enono-1,5-la ctone (2), readily prepared from D-glucosamine, undergoes a rearrangement on treatment with tin(IV) chloride which leads to 3-acetamido-2-pyrone (3) and 2-acetamido-2,3-dideoxy-4,6-O-formylidene-D-threo-hex-2-enono-1,5-lact one (4). A mechanism is proposed for this unusual rearrangement, which was not observed for other analogous hex-2-enono-1,5-lactones. For example, the 2-acetoxy analog of 2 (2-acetoxy-4,6-O-benzylidene-3-deoxy-D-erythro-hex-2-enono-1,5-lactone , 7) was synthesized and treated with tin(IV) chloride affording 3-acetoxy-6-chloromethyl-2-pyrone (8) as main product. The 2-pyrone derivatives 3 and 4 are convenient precursors for the synthesis of 5-hydroxynorvaline (12) and (2S,4R,5R)-4,5,6-trihydroxynorleucine (14), respectively. The latter was prepared by diastereoselective hydrogenation of 4, followed by deprotection.  |l eng 
536 |a Detalles de la financiación: Universidad de Buenos Aires, EX-173 
536 |a Detalles de la financiación: Acknowledgements. We thank the University of Buenos Aires (grant EX-173) and CONICET (Consejo National de Investigaciones Cientificas y Tecnicas) for financial support, and UMYMFOR (CONICET-FCEN-UBA) for the microanalyses. 0. V. and R. M. L. are Research Members of CONICET. 
593 |a Depto. de Quimica Orgánica, Fac. de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón II, 1428, Buenos Aires, Argentina 
690 1 0 |a 4,5,6 TRIHYDROXYNORLEUCINE 
690 1 0 |a 5 HYDROXYNORVALINE 
690 1 0 |a AMINO ACID DERIVATIVE 
690 1 0 |a UNCLASSIFIED DRUG 
690 1 0 |a ARTICLE 
690 1 0 |a CHIRALITY 
690 1 0 |a DRUG SYNTHESIS 
690 1 0 |a NUCLEAR MAGNETIC RESONANCE 
690 1 0 |a PRIORITY JOURNAL 
690 1 0 |a REACTION ANALYSIS 
690 1 0 |a TECHNIQUE 
700 1 |a De Lederkremer, R.M. 
700 1 |a Varela, O. 
773 0 |d Elsevier Ltd, 1996  |g v. 52  |h pp. 12911-12918  |k n. 40  |p TETRAHEDRON  |x 00404020  |w (AR-BaUEN)CENRE-45  |t Tetrahedron 
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