- A General Amino Acid Synthesis Enabled by Innate Radical Cross-Coupling
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The direct union of primary, secondary, and tertiary carboxylic acids with a chiral glyoxylate-derived sulfinimine provides rapid access into a variety of enantiomerically pure α-amino acids (>85 examples). Characterized by operational simplicity, this radical-based reaction enables the modular assembly of exotic α-amino acids, including both unprecedented structures and those of established industrial value. The described method performs well in high-throughput library synthesis, and has already been implemented in three distinct medicinal chemistry campaigns.
- Ni, Shengyang,Garrido-Castro, Alberto F.,Merchant, Rohan R.,de Gruyter, Justine N.,Schmitt, Daniel C.,Mousseau, James J.,Gallego, Gary M.,Yang, Shouliang,Collins, Michael R.,Qiao, Jennifer X.,Yeung, Kap-Sun,Langley, David R.,Poss, Michael A.,Scola, Paul M.,Qin, Tian,Baran, Phil S.
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supporting information
p. 14560 - 14565
(2018/10/24)
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- Preparation method N-t-butyloxycarboryl morpholine-3-carboxylic acid
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The invention provides a preparation method of N-t-butyloxycarboryl morpholine-3-carboxylic acid. According to the preparation method, 1,2-epoxypropane is taken as a raw material, ring-opening reaction, cyclization reaction, hydrolysis reaction, and nitrogen protection reaction are carried out successively so as to obtain N-t-butyloxycarboryl morpholine-3-carboxylic acid, wherein the ring-openingreaction is carried out under catalytic effect of transition metal Lewis acid. Reaction conditions are mild; operation is simple; no severely toxic side product is generated; the reaction yield of each step is 80% or higher; the reaction yield of a part reaction steps is 90% or higher; the yield is high; the preparation method is beneficial for large scale production, and is high in market value.
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- Synthesis of 3-oxadiazolyl/triazolyl morpholines: Novel scaffolds for drug discovery
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Synthesis of isomeric 3-oxadiazolyl/triazolyl morpholines was performed based on a common intermediate on the gram scale. The target compounds were designed as novel scaffolds for the medicinal chemistry. The key reaction was an electrochemical CH-oxidati
- Tereshchenko, Alexander D.,Myronchuk, Julia S.,Leitchenko, Lena D.,Knysh, Irina V.,Tokmakova, Ganna O.,Litsis, Olena O.,Tolmachev, Andrey,Liubchak, Konstantin,Mykhailiuk, Pavel
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p. 750 - 757
(2017/01/16)
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- ANTI-INFECTIVE COMPOUNDS
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The present invention relates to small molecule compounds having the general formula (I): wherein A is a moiety selected from the group consisting of formulae (A) to (K) and their use in the treatment of bacterial infections, in particular Tuberculosis.
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- SUBSTITUTED MORPHOLINES AS MODULATORS FOR THE CALCIUM SENSING RECEPTOR
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Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).
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Paragraph 0351
(2014/02/15)
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- SUBSTITUTED MORPHOLINES AS MODULATORS FOR THE CALCIUM SENSING RECEPTOR
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Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (Ca SR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (Ca SR) receptors of Formula (I).
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Page/Page column 57
(2012/09/22)
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- BETA CARBOLINES AND USES THEREOF
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This invention provides beta-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, G, and x are as described in the specification. The compounds are useful for treating cancer and inflammatory disorders.
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Page/Page column 46-47
(2009/06/27)
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- POLYHETEROCYCLIC COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS
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The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, X5, X6, R1, R2, R3, m, n, and p are as defined as in formula (I), or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
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Page/Page column 40
(2010/02/13)
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- NEW COMPOUNDS
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The present invention relates to new compounds of formula I, wherein P Q X1 X2 X3 X4 X5 R R1 R2 R3 R4R5 G M1 M2 M3 m and n are defined as in formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
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- N-heterocyclic derivatives as NOS inhibitors
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N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
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