- Palladium-Catalyzed Reductive Carbonylation of (Hetero) Aryl Halides and Triflates Using Cobalt Carbonyl as CO Source
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An efficient protocol for the reductive carbonylation of (hetero) aryl halides and triflates under CO gas-free conditions using Pd/Co2(CO)8 and triethylsilane has been developed. The mild reaction conditions, enhanced chemoselectivity and, easy access to heterocyclic and vinyl carboxaldehydes highlights its importance in organic synthesis.
- Dogga, Bhushanarao,Joseph, Jayan T.,Kumar, C. S. Ananda
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supporting information
p. 309 - 313
(2020/12/23)
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- Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters
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The 3C-like protease (3CLpro), which controls the severe acute respiratory syndrome (SARS) coronavirus replication, has been identified as a potential target for drug design in the treatment of SARS. A series of tetrapeptide phthalhydrazide ketones, pyridinyl esters, and their analogs have been designed, synthesized, and evaluated as potential SARS 3CLpro inhibitors. Some pyridinyl esters are identified as very potent inhibitors, with IC50 values in the nanomolar range (50-65 nM). Electrospray mass spectrometry indicates a mechanism involving acylation of the active site cysteine thiol for this class of inhibitors.
- Zhang, Jianmin,Pettersson, Hanna I.,Huitema, Carly,Niu, Chunying,Yin, Jiang,James, Michael N. G.,Eltis, Lindsay D.,Vederas, John C.
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p. 1850 - 1864
(2008/02/02)
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- Enantioselective synthesis of (S)-3-(4-thiazolyl)-2-tert- butoxycarbonylaminopropionic acid: A chiral building block for renin inhibitor
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(S)-3-(4-Thiazolyl)-2-tert-butoxycarbonylaminopropionic acid (6), an important structural constituent of the renin inhibitor, has been synthesized from (Z)-3-(4-thiazolyl)-2-benzoylaminoprop-2-enoic acid (4b) by enantioselective hydrogenation using the Ru
- Yuasa, Yoshifumi,Tsuruta, Haruki,Yuasa, Yoko
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p. 2385 - 2392
(2007/10/03)
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- 5-THIAZOLE SUBSTITUTED 2-PYRROLIDINE-CARBOXYLIC ACIDS
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Anti-viral agents of Formula (1a) wherein: RA represents hydroxy; RB represents 4-tert-butylbenzoyl further substituted in the meta-position by halo or C1-3alkoxy; RC represents 2-thiazolyl, 5-methylthiazol-2-yl
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- A New Convenient Preparation of 2-, 4-, and 5-Thiazolecarboxaldehydes and Their Conversion into the Corresponding Carbonitrile N-Oxides: Synthesis of 3-Thiazolylisoxazoles and 3-Thiazolylisoxazolines
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The title aldehydes are prepared in high yields by quenching 2-lithiothiazole, 4-lithio-, and 5-lithio-2-trimethylsilylthiazole with N-formylmorpholine followed by protodesilylation in the latter two cases.The aldehydes are transformed through their oxime
- Dondoni, Alessandro,Fantin, Giancarlo,Fogagnolo, Marco,Medici, Alessandro,Pedrini, Paola
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p. 998 - 1001
(2007/10/02)
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- Electrophilic Aromatic Reactivities via Pyrolysis of Esters. Part 21. ?+ Values for Thiazole : the High Polarisability of Thiazole, and the Effect of Hydrogen Bonding on the Reactivity of N-Containing Heterocycles
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The rates of gase-phase elimination of acetic acid from 1-arylethyl acetates (aryl = thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, or phenyl) have been measured between 633.2 and 698.5 K.The relative rates of pyrolysis at 650 K are : thiazol-2-yl, 0.271; thia
- August, Ryan,Davis, Carole,Taylor, Roger
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p. 1265 - 1268
(2007/10/02)
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- N-aminomethyl-2-amino(and 2-amino-methyl)-2-(2-quinolyl)-thioacetamides
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The compounds are N-aminomethyl-2-amino(and 2-aminomethyl)-2-heterocyclic-thioacetamides which are inhibitors of gastric acid secretion.
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- 2-Alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides
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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.
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