- Cascade Trisulfur Radical Anion (S3?-) Addition/Electron Detosylation Process for the Synthesis of 1,2,3-Thiadiazoles and Isothiazoles
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Trisulfur radical anion (S3?-) mediated reactions with in situ formed azoalkenes and α,β-usaturated N-sulfonylimines for the construction of 1,2,3-thiadiazoles and isothiazoles has been developed. S3?- is in situ generated from potassium sulfide in DMF. These two approaches provide a new, safe, and simple way to construct 4-subsituted 1,2,3-thiadiazoles, 5-subsituted 1,2,3-thiadiazoles, and isothiazole in good yields. The reactions include the formation of the new C-S and N-S bonds via S3?- addition and electron detosylation under mild conditions.
- Liu, Bei-Bei,Bai, Hui-Wen,Liu, Huan,Wang, Shun-Yi,Ji, Shun-Jun
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p. 10281 - 10288
(2018/07/25)
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- NEW ARYLALKENYLPROPARGYLAMINE DERIVATIVES EXHIBITING NEUROPROTECTIVE ACTION FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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The invention relates to novel arylalkenylpropargylamine derivatives of general formula (I) or enantiomers or diastereomers thereof or salts, optionally pharmaceutically acceptable salts, or solvates of any of these. The compounds can be used in treating or preventing a disease or condition in a mammal related to monoamine oxidase dysfunction, especially in neurodegenerative diseases, e.g. Parkinson's disease, Alzheimer's disease or Huntington's disease.
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Page/Page column 55
(2015/06/25)
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- PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES OF OMARIGLIPTIN
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Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of the active pharmaceutical ingredient named Omarigliptin.
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Paragraph 0079
(2015/11/11)
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- One-step synthesis of α-Chloro acetophenones from acid chlorides and Aryl precursors
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A direct and efficient method was developed for the preparation of a variety of substituted acetophenone derivatives from readily available arene precursors and acid chlorides. This method has significant generality and affords access to substitution patt
- Rosen, Jonathan,Steinhuebel, Dietrich,Palucki, Michael,Davies, Ian
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p. 667 - 669
(2008/02/05)
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- Asymmetric zinc-Reformatsky reaction of Evans chiral imide with acetophenones and its application to the stereoselective synthesis of triazole antifungal agents
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The Ni(acac)2 catalytic ZnEt2-mediated asymmetric Reformatsky-type reaction of Evans chiral imide with various acetophenones was studied. The chiral imido zinc enolate, which was formed through the metal-halogen exchange reaction of
- Yu, Luo-Ting,Ho, Meng-Tsung,Chang, Ching-Yao,Yang, Teng-Kuei
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p. 949 - 962
(2008/02/03)
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