- CRYSTAL OF CYCLIC PHOSPHONIC ACID SODIUM SALT AND METHOD FOR MANUFACTURING SAME
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An object of the present invention is to provide a crystal of a cyclic phosphonic acid sodium salt (2ccPA) with high purity and excellent storage stability and a method for producing the crystal. The present invention provides a crystal of a cyclic phosphonic acid sodium salt (2ccPA) represented by formula (1):
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Paragraph 0356; 0357; 0358; 0359; 0360; 0361
(2017/09/02)
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- 3,5-Disubstituted pyranone analogues of highly antifungally active furanones: Conversion of biological effect from antifungal to cytostatic
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A series of 3-aryl-5-acyloxymethyl-5,6-dihydro-2H-pyran-2-ones, related to highly antifungally active butenolides, was synthesized via cyclization of substituted δ-hydroxy acids as the key step, and evaluated for their in vitro antifungal activity and cytostatic activity. While the extension of the furanone ring to pyranone led to a complete loss of the antifungal effect, some of the compounds displayed promising effect against several cell lines, including the resistant colorectal carcinoma cells.
- Schiller, Radan,Tichotová, Lucie,Pavlík, Jan,Buchta, Vladimír,Melichar, Bohuslav,Votruba, Ivan,Kune?, Ji?í,?pulák, Marcel,Pour, Milan
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p. 7358 - 7360
(2011/01/12)
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- Synthetic studies on spiroketal natural products. IV. A stereoselective synthesis of (3S,5S,6R,9R,R(S))-3-benzyloxymethyl-9-hydroxymethyl-5-(p-tolyl)sulfin yl-1,7-dioxaspiro[5.5]undecane, a key intermediate for talaromycins
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A dioxaspiro compound (4), a common intermediate for the synthesis of talaromycin A (1) and (-)-talaromycin B (2), was synthesized by two routes utilizing two kinds of asymmetric recognition of prochiral 1,3-diols controlled by sulfinyl chirality, that is, firstly by acid promoted diastereoselective C-O bond fission of the bicyclic acetal (7) to give the dihydropyran derivative (6), which has an S-hydroxymethyl group at the C3-position (7 → 6), and secondly by diastereoselective intramolecular Michael addition of the diol (5), in which the three chiral centers at C5, C6, C9 were constructed in one step (5 → 4).
- Iwata,Maezaki,Hattori,Fujita,Moritani,Takemoto,Tanaka,Imanishi
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p. 339 - 345
(2007/10/02)
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- SYNTHESIS OF 5,5'-DIHYDROXYLEUCINE AND 4-FLUORO-5,5'-DIHYDROXYLEUCINE, THE REDUCTION PRODUCTS OF 4-CARBOXYGLUTAMIC AND 4-CARBOXY-4-FLUOROGLUTAMIC ACIDS
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Schemes for the synthesis of 5,5'-dihydroxyleucine 3 and its 4-fluoro analog 7 involving the condensation of a suitable 'aminoacid moiety' with 2,2-dimethyl-5-iodomethyl-1,3-dioxane 15D or its fluoro analog 27A were tested.The anion of the ethyl N-diphenylmethylene-glycinate 25 gave better yields of 3 than the classical anion of diethyl acetamidomalonate.This strategy could not be successfully applied to the synthesis of 7, which could be prepared by reduction of a suitably protected 4-fluoro-4-carboxyglutamate with BMS.
- Dubois, Joelle,Foures, Christine,Bory, Sonia,Falcou, Serge,Gaudry, Michel,Marquet, Andree
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p. 1001 - 1012
(2007/10/02)
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- ASYMMETRIC FUNCTIONALIZATION AT A PROCHIRAL CARBON CENTER BY THE AID OF SULFINYL CHIRALITY: A SELECTIVE FORMATION OF 6-SUBSTITUTED (3R,SS)- AND (3S,SS)-3-HYDROXYMETHYL-3,4-DIHYDRO-5-(p-TOLYL)SULFINYL-2H-PYRANS
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A successful asymmetric functionalization of prochiral gem-bis(hydroxymethyl) groups has been achieved by the aid of a sulfinyl chirality.
- Iwata, Chuzo,Fujita, Masahiro,Moritani, Yasunori,Sugiyama, Kenji,Hattori, Kohji,Imanishi, Takeshi
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p. 3131 - 3134
(2007/10/02)
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- DIASTEREOTOPIC GROUP SELECTIVITY AT A PROSTEREOGENIC CARBON CENTER: SYNTHESIS OF (+/-)-SYN-4,8-DIMETHYLDECANAL
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A group selective dealkylation reaction of a bridged ketal with trimethylsilyl iodide serves to control stereochemistry at carbon centers that are separated by five atoms.In combination with the iron/copper promoted fragmentation reaction of a hydroperoxi
- Schreiber, Stuart L.,Hulin, Bernard
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p. 4561 - 4564
(2007/10/02)
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