- A new method for the preparation of (2R)-2-amino-5-phosphonopentanoic acid
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A new and efficient synthesis of (2R)-2-amino-5-phosphonopentanoic acid(AP5) is reported. Our approach is based on a pseudo-Claisen [2,3] sigmatropic rearrangement of an alkyne phosphite.
- Muller,Mann,Taddei
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- Asymmetric synthesis of D-(E)-2-amino-5-phosphono-3-pentenoic acid (APPA) by using a chiral auxiliary
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The synthesis of D-2-amino-5-phosphono-3-pentenoic acid (1) is reported. The key intermediate, a (2R,3S)-3-hydroxyallylglycine derivative (8), was prepared by the reaction of (5S)-3,6-dimethoxy-5-isopropyl-2,4-dihydropyrazine (2) and acrolein in the presence of chlorotitanium tris(diethylamide). The transformation of 8 into 1 via allylic alcohol 11 was carried out by following the reported route.
- Fukuari, Masashi,Ichimoto, Itsuo,Kirihata, Mitsunori
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- Involucrin gene expression promoter
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PROBLEM TO BE SOLVED: To provide an involucrin gene expression promoter that has high effect of promoting involucrin gene expression, and is applied to the skin, to quickly increase involucrin concentrations, and markedly improving the barrier function. SOLUTION: An involucrin gene expression promoter contains at least one selected from a compound represented by the following formula (1) [where R1 and R2 are the same or different to represent a hydrogen atom, or a substituent. n is an integer of 1 or greater], a salt thereof, and their hydrates as an active ingredient. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPO&INPIT
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Paragraph 0097; 0101
(2019/03/28)
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- Phosphorus-containing aminocarboxylic acids. VI. Improved synthesis of 2-amino-5-phosphonopentanoic acid
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An improved three-step procedure for the synthesis of 2-amino-5-phosphonopentanoic acid is proposed.
- Rozhko,Ragulin,Tsvetkov
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p. 1065 - 1067
(2007/10/03)
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- Phosphorus-containing aminocarboxylic acids. VII. Asymmetric synthesis of ω-phosphono-α-aminocarboxylic acids
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New asymmetric ω-phosphono-α-aminocarboxylic acids were synthesized by alkylation with ω-bromoalkylphosphonates of the glycine methylene group in the Ni(II) complex of the Schiff base derived from glycine and (S)- and (R)-2-N-(N-benzylprolyl)-o-aminobenzo
- Andronova,Maleev,Ragulin,Il'in,Tsvetkov,Belokon'
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p. 1068 - 1071
(2007/10/03)
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- Highly enantioselective synthesis of (R)- and (S)-2-amino-5-phosphonopentanoic acids [(R)- and (S)-AP5] via modified Seebach imidazolidinones
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The preparation of four new stereoisomeric 1-carbobenzyloxy-2-tert-butyl-3-(α-methylbenzyl)-1,3-imidazolidin-4-o nes is described. Alkylation of the lithium enolates of these chiral glycine derivatives proceeds with high diastereoselectivity. In particula
- Garcia-Barradas, Oscar,Juaristi, Eusebio
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p. 3423 - 3434
(2007/10/02)
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