93204-36-5Relevant articles and documents
HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ABNORMAL CELLULAR PROLIFERATION
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Page/Page column 127-128, (2019/07/20)
This invention is in the area of heterocyclic-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Tetrahydroisoquinoline intermediate of compound preparation method
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Paragraph 0100; 0101; 0102; 0103; 0104, (2017/08/25)
The invention provides a tetrahydroisoquinoline compound with the following structural general formula I. The invention also provides application of the above tetrahydroisoquinoline compound as an intermediate for the preparation of tetrahydroisoquinoline alkaloid natural medicaments. The invention further provides a method for preparing the tetrahydroisoquinoline compound. The method uses a halogenated aromatic compound as a starting material, and conducts nucleophilic substitution, addition, hydroxy elimination and protecting group elimination reaction, thereby obtaining the tetrahydroisoquinoline compound with chiral amine.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000299, (2015/04/15)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
DIPEPTIDE AND TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
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Paragraph 00311; 00312, (2014/10/04)
Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.
Lewis acid facilitated regioselective synthesis of τ-histidinoalanine
Wu, Ju,Ma, Bing,Wang, Yuehui,Zhang, Yue,Yan, Shenghu,Castle, Steven L.
, p. 3114 - 3116 (2014/05/20)
τ-Histidinoalanine, with an unusual cross-link between His and Ala, is the central component of theonellamides, a family of bioactive peptidic natural products. Previous syntheses of this residue were plagued with low regioselectivity in the alkylation step. Herein, we report two novel routes to τ-histidinoalanine, involving alkylation of Boc-His-OMe with a serine-derived β-lactone and β-bromoalanine, respectively, as the electrophiles. The use of Mg(OTf)2 as a catalyst was found to be essential to ensure high regioselectivity for the τ-isomer, presumably due to the formation of a six-membered ring chelation involving the π-nitrogen atom of histidine.
A mild and efficient chemoselective: N-benzyloxycarbonylation of amines using TBAB a catalyst under solvent-free conditions
Babu, Kothamasu Suresh,Rao, Vidadala Rama Subba,Rao, Ravu Ranga,Babu, Sakhamuri Sivaram,Rao, Janaswami Madhusudana
experimental part, p. 393 - 396 (2009/10/17)
We describe a mild and efficient method for the chemoselective N-benzyloxycarbonylation of amines by treatment amines and aminoesters with benzyloxycarbonyl chloride (Cbz-Cl) in the presence of TBAB under solvent-free in excellent yields. The method is ge
4,4-Difluorinated analogues of l-arginine and NG-hydroxy-l-arginine as mechanistic probes for nitric oxide synthase
Martin, Nathaniel I.,Woodward, Joshua J.,Winter, Michael B.,Marletta, Michael A.
supporting information; experimental part, p. 1758 - 1762 (2009/11/30)
4,4-Difluoro-l-arginine and 4,4-difluoro-NG-hydroxy-l-arginine were synthesized and shown to be substrates for the inducible isoform of nitric oxide synthase (iNOS). Binding of both fluorinated analogues to the NOS active site was also investigated using a spectral binding assay employing a heme domain construct of the inducible NOS isoform (iNOSheme). 4,4-Difluoro-NG-hydroxy-arginine was found to bind at the NOS active site in a unique manner consistent with a model involving ligation of the FeIII heme center by the oxygen atom of the NG-hydroxy moiety.
Rearrangement of N-alkyl 1,2-amino alcohols. Synthesis of (S)-toliprolol and (S)-propanolol
Duthion, Béranger,Métro, Thomas-Xavier,Gomez Pardo, Domingo,Cossy, Janine
experimental part, p. 6696 - 6706 (2011/02/26)
N-alkyl 1,2-amino alcohols were rearranged stereospecifically by using TFAA/Et3N. This rearrangement has been used to synthesize N-isopropyl-3-(aryloxy)-2-hydroxypropylamines, β-adrenergic blocking agents such as (S)-toliprolol and (S)-propanolol.
Mild and chemoselective deacetylation method using a catalytic amount of acetyl chloride in methanol
Yeom, Chang-Eun,Lee, So Young,Kim, Young Jong,Kim, B. Moon
, p. 1527 - 1530 (2007/10/03)
Efficient deacetylation of alcohol acetates under mild acidic conditions was accomplished with a catalytic amount of acetyl chloride in methanol. Acetates of various primary, secondary, aromatic and sugar alcohols were successfully deprotected. Highly chemoselective removal of acetyl groups in presence of other commonly employed esters was also achieved in excellent yields. The reactivity of this transesterification-mediated deacetylation was found to be directly dependent upon the electronic and steric nature of the acetates. Georg Thieme Verlag Stuttgart.
Enantioselective synthesis of protected D-serine from tetrahydrooxazin-4-one via a hetero Diels-Alder reaction
Panunzio, Mauro,Bandini, Elisa,Campana, Eileen,Vicennati, Paola
, p. 2113 - 2115 (2007/10/03)
Hetero Diels-Alder reaction between 2-aza-3-trimethylsilyloxy-1,3-diene and aldehydes gives rise to tetrahydrooxazin-4-ones, useful intermediates in the synthesis of α-amino-β-hydroxy acids. Herein we report the complete stereoselective synthesis of D-serine Cbz-methyl ester.
