- SuFExable Isocyanides for Ugi Reaction: Synthesis of Sulfonyl Fluoro Peptides
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Herein, the sulfonyl fluoro isocyanides were first developed as a new type of SuFExable synthon, and they are used as building blocks in the Ugi reaction (U-4CR). The Ugi reaction was established and the substrate scope was investigated, and various sulfonyl fluoro α-amino amides and peptides could be reached in a one-step synthesis. Therefore, this protocol opens a new vision for SuFExable building blocks and click chemistry, and it also provides a distinct approach to sulfonyl fluoro peptides.
- Xu, Shuheng,Cui, Sunliang
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p. 5197 - 5202
(2021/07/20)
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- INHIBITING UBIQUITIN SPECIFIC PEPTIDASE 30
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The present disclosure relates to chemical entities useful as inhibitors of Ubiquitin Specific Peptidase 30 (USP30), pharmaceutical compositions comprising the chemical entities, and methods of using the chemical entities. The chemical entities as disclosed herein can be useful in the treatment of a disease, disorder, or condition involving mitochondrial dysfunction, including neurodegenerative diseases, motor neuron diseases, metabolic disorders, and cancers, among other ailments.
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Paragraph 00192; 00215
(2019/04/30)
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- Synthesis of (-)-dihydropinidine, (2S,6R)-isosolenopsin and (+)-monomorine via a chiral synthon from l-aspartic acid
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The use of a β-amino aldehyde derived from l-aspartic acid as a chiral synthon to construct 2,6-disubstituted piperidines is described. The synthesis of (-)-dihydropinidine·HCl, (2S,6R)-isosolenopsin·HCl and (+)-monomorine has been achieved from this chiral synthon using a Wittig reaction followed by hydrogenation (reductive cyclization) as the key steps.
- Reddy, Chada Raji,Latha, Bellamkonda
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p. 1849 - 1854
(2012/02/05)
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
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Page/Page column 57
(2010/11/27)
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
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Page/Page column 268-270
(2008/06/13)
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- Useful synthesis of 2,3,6-tri- and 2,3,5,6-tetrasubstitutedpyridine derivatives from aspartic acid
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New synthetic methods for 2,3,6-tri- and 2,3,5,6-tetrasubstituted pyridineskeletons, which are the essential main central segments of thiostrepton-type macrocyclic antibiotics, were developed from l-α-aspartic acid (Asp) via the Asp-derived α-dehydroamino
- Yonezawa, Yasuchika,Konn, Akihito,Shin, Chung-gi
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p. 2735 - 2746
(2007/10/03)
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- Manipulating L-aspartic and L-glutamic acids - Diastereoselective synthesis of enantiopure β-amino-γ-hydroxy acids and γ-amino-δ-hydroxy acids
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Enantiopure (3S,4R)- and (3S,4S)-3-amino-4-hydroxyhexanoic acids and (4S,5R)- and (4S,5S)-4-amino-5-hydroxyheptanoic acid derivatives have been prepared by stereodivergent synthesis from L-aspartic and L-glutamic acids, respectively. The stereochemistry at the carbon atom attached to the amino group was determined from the starting material but the configuration at C-4 or C-5 is controlled by diastereoselective alkylation with diethylzinc or ethylmagnesium bromide. The protection of the carboxylic group as OBO orthoester improved the yields in the final products. Wiley-VCH Verlag GmbH & Co, KGaA, 69451 Weinheim, Germany, 2003.
- Andres, Jose M.,Munoz, Eva M.,Pedrosa, Rafael,Perez-Encabo, Alfonso
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p. 3387 - 3397
(2007/10/03)
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- Enantioselective synthesis of 2-isocephem and 2-isooxacephem antibiotics
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The azido lactone 8 was prepared in a highly stereoselective manner by introduction of an azide function to the lactone 6 derived from L-aspartic acid, and then was converted into (2S,3S)-3-amino-2-azido-4-hydroxybutanoic acid 4. Four-component condensation of the amino acid 4, p-nitrobenzyl isocyanide and formaldehyde or 2,2-diethoxyacetaldehyde furnished the corresponding 3,4-cis-azetidinone 16 or 26 in excellent yield. 3-Methoxy-2-isooxacephalosporin was prepared by the intramolecular acylation of imidazolide 23 derived from compound 16. 3-Unsubstituted 2-isocephem and 2-isooxacephem analogues were prepared from the azetidinone 26.
- Nitta, Hajime,Ueda, Ikuo,Hatanaka, Minoru
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p. 1793 - 1798
(2007/10/03)
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- The total synthesis of L-daunosamine
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N,O-Dibenzyl-N-tert-butoxycarbonyl-L-homoserinal (7), obtained from L-aspartic acid, reacts with vinylmagnesium chloride to afford with high stereoselectivity compound 6 which is subsequently transformed into the derivative of L
- Jurczak, Janusz,Kozak, Janusz,Golebiowski, Adam
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p. 4231 - 4238
(2007/10/02)
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