- METHODS OF MAKING HIGH ENANTIOSELECTIVE SECONDARY ALCOHOLS
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A new process to synthesis of compound OBI-3424 R-form and S-form products is provided. The "R-form" compound OBI-3423 was first synthesized with 48% overall yield from compound OBI-3424-5 by installation of the labile phosphate motif at later stage. The stereo chemistry is established by 5 steps chemo-enzyme combination synthesis to afford 99% optical purity, After then, the "S-form" compound OBI-3424 is prepared with improving overall yield of 54% from compound OBI-3424-5. The stereo chemistry is established by 4 steps combination of chemo-enzyme synthesis with excellent optical purity of 99%.
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Paragraph 0074; 0075
(2020/09/08)
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- Tripterygium wilfordii derivative and application
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The invention relates to a tripterygium wilfordii derivative, preparation and application thereof. The tripterygium wilfordii derivative has a molecular formula shown as the specification. Compared with the prior art, the tripterygium wilfordii derivative
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Paragraph 0039; 0041; 0046; 0048
(2019/07/04)
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- Camptothecin derivative with antitumor activity, and preparation method and application thereof
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The present invention relates to a camptothecin derivative with antitumor activity, and a preparation method and an application thereof. The camptothecin derivative is a compound having a structure represented by general formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a tautomer, a solvate, a polymorph or a prodrug thereof. The camptothecin derivative has a goodantitumor cell proliferation activity, has an inhibitory activity against specific tumor cells at a very low concentration, and has excellent selectivity; and the side effects of the camptothecin derivative represented by the general formula (I) are greatly less than those of Tripterygium wilfordii Hook. f., so the camptothecin derivative can be used to treat specific tumors.
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Paragraph 0105; 0107; 0111; 0113; 0118; 0120; 0124; 0126
(2019/11/04)
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- Amidation reaction of carboxylic acid with formamide derivative using SO3?pyridine
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The amidation reaction of carboxylic acid derivatives was developed using sulfur trioxide pyridine complex (SO3?py) as a commercially available and easily handled oxidant. This method could be applied to the reaction of various aromatic and aliphatic carboxylic acids, including optically active ones, with formamide derivatives to afford the corresponding amides in good to high yields.
- Kawano, Shota,Saito, Kodai,Yamada, Tohru
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supporting information
p. 584 - 586
(2018/04/12)
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- Bifunctional organocatalysts for the asymmetric synthesis of axially chiral benzamides
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Bifunctional organocatalysts bearing amino and urea functional groups in a chiral molecular skeleton were applied to the enantioselective synthesis of axially chiral benzamides via aromatic electrophilic bromination. The results demonstrate the versatilit
- Miyaji, Ryota,Wada, Yuuki,Matsumoto, Akira,Asano, Keisuke,Matsubara, Seijiro
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supporting information
p. 1518 - 1523
(2017/08/14)
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- (R)- AND (S)-1-(3-(3-N,N-DIMETHYLAMINOCARBONYL)PHENOXYL-4-NITROPHENYL)-1-ETHYL-N,N'-BIS (ETHYLENE)PHOSPHORAMIDATE, COMPOSITIONS AND METHODS FOR THEIR USE AND PREPARATION
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Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of
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Paragraph 0073-0074
(2017/06/12)
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- NOVEL TRIAZINE COMPOUNDS
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The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/ or the mTOR pathway.
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Page/Page column 68-69
(2012/08/08)
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- 2-(3,5-DISUBSTITUTEDPHENYL)PYRIMIDIN-4(3H)-ONE DERIVATIVES
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O N NH R3 R2 O R1 168 ABSTRACT The present invention provides a 2-(3,5-disubstitutedphenyl)pyrimidin- 4(3H)-one compound of Formula (I) 5 (I) or a pharmaceutically acceptable salt thereof wherein R 1, R2 and R3 are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and 10 the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.
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Page/Page column 75
(2012/01/06)
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- REGIOSELECTIVE METALLATIONS OF (METHOXYMETHOXY)ARENES
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The methoxymethoxy substituent when attached to an aromatic ring functions as a moderately strong ortho-directing group in hydrogen-metal exchenge reactions.In many cases the propensity of the methoxymethoxylated arene toward ring metallations is greatly enhanced with concomitant suppression of undesirable side reactions such as nucleophilic attack and addition of metallating species.Unlike many other ortho-directing groups, the regio-direction of the methoxymethoxy substituent when in conjunction with other weaker directing groups is dependent upon the metallating medium.Thus, by changing the electron donating capacity of the metallating medium it is possible to selectively direct metallation to either of the positions ortho to the methoxymethoxy substituent.
- Ronald, Robert C.,Winkle, Mark R.
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p. 2031 - 2042
(2007/10/02)
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