- METHODS OF TREATMENT WITH AMINOLEVULINIC ACID SYNTHASE 2 (ALAS2) MODULATORS
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Described herein is a compound of Formula I or a pharmaceutically acceptable salt thereof: wherein Ring A R1, R2, a, b, and n are as defined herein. Also described is a method of treating a subject having a disorder in need of treatment, comprising inhibiting aminolevulinic acid synthase 2 (ALAS2) in the subject by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Disorders that are of particular interest are blood disorders, such as porphyria and anemia.
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Paragraph 00157
(2020/12/29)
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- Synthesis of boronophenylalanine-like aza-amino acids for boron-containing azapeptide precursors
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Aza-amino acids and an azapeptide with a boron-containing substituent were developed for the first time. We synthesized p-boronophenylalanine (BPA)-like aza-amino acid (aza-BPA) and its analogs in which the α-carbon of the peptide is replaced by nitrogen and the boronate ester is situated at the ortho, meta, or para position of the phenyl group. The N- and C-terminals of aza-BPA were linked to α-amino acids to afford an α/aza/α-tripeptide. These compounds are expected to be used in boron neutron capture therapy, chemotherapy, and synthesis of functional materials.
- Miyata, Kota,Narita, Airi,Fujisawa, Ryota,Roppongi, Makoto,Ito, Satoshi,Shingo, Tamesue,Oba, Toru
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- PROCESS FOR THE SYNTHESIS OF BETA-AMINOCARBONYLS
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The present application provides processes and intermediates useful in the production of β- aminocarbonyl- or β-aminothiocarbonyl-containing compounds. Provided herein is a process for synthesizing β-aminocarbonyl- or β-aminothiocarbonyl-containing compounds from an alkene and a hydrazone. Also provided herein is a process for synthesizing β-aminocarbonyl- or β-aminothiocarbonyl-containing compounds from an alkene and a hydrazine. The present application further provides intermediate aminoisocyanate and iminoisocyanate compounds, and methods for synthesizing the starting hydrazone and hydrazine compounds.
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Paragraph 00100
(2013/05/23)
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- Synthesis of hydrazine and azapeptide derivatives by alkylation of carbazates and semicarbazones
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Hydrazine and azapeptide analogs were synthesized effectively by alkylation of alkylidene carbazates and semicarbazones. In comparisons of benzylidene, benzhydrylidene, and fluorenylidene tert-butyl carbazates in alkylations using bases of different pKb character, superior conversion was obtained using the fluorenone derivative. Mild alkylation conditions were found employing Et4NOH as base and used to convert fluorenylidene tert-butyl carbazate into 13 different protected hydrazines. Moreover, racemization was avoided during alkylation of fluorenylidene semicarbazide in the synthesis of aza-propargylglycinylphenylalanine tert-butyl ester, the protecting groups from which could be selectively removed.
- Garcia-Ramos, Yesica,Proulx, Caroline,Lubell, William D.
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p. 985 - 993
(2013/02/22)
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- A tunable route for the synthesis of azomethine imines and β-aminocarbonyl compounds from alkenes
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Cyclic azomethine imines possessing a β-aminocarbonyl motif are accessed from simple alkene and hydrazone starting materials. A thermal, concerted alkene aminocarbonylation pathway involving an imino-isocyanate intermediate is proposed and supported by DF
- Clavette, Christian,Gan, Wei,Bongers, Amanda,Markiewicz, Thomas,Toderian, Amy B.,Gorelsky, Serge I.,Beauchemin, Andre M.
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supporting information
p. 16111 - 16114,4
(2020/09/09)
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- Phase-transfer catalytic aza-Michael addition of tert-butyl benzyloxycarbamate to electron-deficient olefins
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A highly efficient phase-transfer catalytic aza-Michael addition of tert-butyl benzyloxycarbamate to a wide range of electron-deficient olefins is presented (90-99%). The Royal Society of Chemistry.
- Lee, Jihoon,Kim, Mi-Hyun,Jew, Sang-Sup,Park, Hyeung-Geun,Jeong, Byeong-Seon
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p. 1932 - 1934
(2008/12/22)
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- Regioselectivity in the Photochemical Ring Contraction of 4-Diazopyrazolidine-3,5-diones to give Aza-β-lactams
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Irradiation of 4-diazopyrazolidine-3,5-diones (15) in the presence of alcohols or water gave mixtures of the isomeric 1,2-diazetidinones (16) and (17), formed by competing photochemical Wolff rearrangement of the two nitrogen groups, followed by reaction of the resulting ketenes with the nucleophile.Some regioselectivity is observed in the ring contraction process, and the relative order of migration of nitrogen groups is NPh>NCHPh2NCH2PhNMe>NCH2CO2Et.The structures of the 1,2-diazetidinones (17c) and (24) were confirmed by X-ray crystallography, and a crystal structure of the diazo compound (15g) was also obtained.Possible reasons for the regioselectivity in the ring contraction are discussed.
- Lawton, Geoffrey,Moody, Christopher J.,Pearson, Christopher J.,Williams, David J.
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p. 885 - 898
(2007/10/02)
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