- Multifunctional immunity-targeted micromolecule anti-cancer medicine (Bestazomib citrate) and preparation method and application thereof
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The invention discloses multifunctional immunity-targeted micromolecule anti-cancer medicine (Bestazomib citrate) and a preparation method and application thereof. A structure of the multifunctional immunity-targeted micromolecule anti-cancer medicine (Be
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Paragraph 0017; 0067; 0068
(2019/01/11)
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- Novel synthesis of (-)-bestatin from L-aspartic acid
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Oxazoline-4-acetate derivative 3 that could be readily obtained from L-aspartic acid was subjected to highly stereoselective hydroxylation, and subsequent Mitsunobu inversion of the hydroxyl group led to (2S,3R)-3-amino-3-benzyl-2-hydroxybutanoic acid der
- Seki, Masahiko,Nakao, Kazuya
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p. 1304 - 1307
(2007/10/03)
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- Ring opening of optically active cis-disubstituted aziridino alcohols: An enantiodivergent synthesis of functionalized amino alcohol derivatives
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Ring-opening reactions of optically active cis-disubstituted aziridino alcohols have been investigated. Regio- and stereo-selective ring opening took place with internal and external nucleophiles. Unusual amino acids derivatives (14) and (15), the key synthetic intermediates for bestatin and related peptides, have been prepared. n.
- Fuji, Kaoru,Kawabata, Takeo,Kiryu, Yoshimitsu,Sugiura, Yukio
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p. 701 - 722
(2007/10/03)
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- An enantiodivergent synthesis of three β-amino alcohols: Preparation of key intermediates for bestatin and the related peptides
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An enantiodivergent method for preparation of three β-amino alcohols and three 1,2-diamines has been developed starting with a chiral aziridine 1. Unusual amino acid derivatives 3 and 5, which are key synthetic intermediates for bestatin and the related peptides, have been prepared.
- Kawabata,Kiryu,Sugiura,Fuji
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p. 5127 - 5130
(2007/10/02)
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- Tributyltin Cyanide, a Novel Reagent for the Stereoselective Preparation of 3-Amino-2-hydroxy Acids via Cyanohydrin Intermediates
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Reaction of tributyltin cyanide with optically active 2-N-benzyloxycarbonylamino aldehydes 1 gives the corresponding O-tributylstannyl cyanohydrins 2 and 3 stereoselectively.Compounds 2 and 3 are transformed in situ into the methyl 3-N-benzyloxycarbonylam
- Herranz, Rosario,Castro-Pichel, Julia,Garcia-Lopez, Teresa
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p. 703 - 706
(2007/10/02)
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- A STEREOCONTROLLED SYNTHESIS OF (-)-BESTATIN FROM AN ACYCLIC ALLYLAMINE BY IODOCYCLOCARBAMATION
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1,2-Asymmetric induction of iodocyclocarbamation is described by using allylamines 2 and 6 and the method has been succesfully applied to a stereocontrolled synthesis of bestatin.
- Kobayashi, Susumu,Isobe, Toshiyuki,Ohno, Masaji
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p. 5079 - 5082
(2007/10/02)
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- Process for producing threo-3-amino-2-hydroxybutanoyl-aminoacetic acids, as well as novel intermediated therefor and process for producing them
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A process for producing threo-3-amino-2-hydroxybutanoylaminoacetic acids comprises the steps of allowing to react a starting compound represented by the general formula: STR1 wherein R1 represents a naphthyl or a group of the formula: STR2 in which R6 and R7 represent individually hydrogen, halogen, amino or a protected amino, hydroxy or a protected hydroxy, a lower alkoxy or a lower alkyl and R2 represents a protected amino, with a starting compound represented by the general formula: STR3 wherein R3 represents hydrogen or an ester residue, to obtain threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its ester represented by the general formula: STR4 wherein R1, R2 and R3 have the same meanings as above, and then reducing the same into threo-3-protected amino-2-hydroxybutanoic acid or its ester represented by the general formula: STR5 wherein R1, R2 and R3 have the same meanings as above, and further converting the above compound into 3-amino-2-hydroxybutanoic acid represented by the general formula: STR6 wherein R2 ' represents amino or a protected amino, thereafter condensing the same, in a conventional manner for forming a peptide coupling, with a compound represented by the general formula: STR7 wherein R4 represents an alkyl having 3-4 carbon atom or 3-guanidinopropyl, while previously protecting as required those groups not relevant to the reaction, and removing the protecting groups for the functional groups to produce threo-3-amino-2-hydroxybutanoylaminoacetic acids represented by the general formula: STR8 wherein R1 and R4 have the same meanings as above. This invention also provides the compounds represented by the general formula (III) as novel intermediates for the above aimed compounds and a process for producing the intermediates.
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