- Photo-sensitized oxy-thiocyanation of terminal alkynes/1,3-aryldienes and their one-pot conversion to 2-hydroxy 4-substituted aryl thiazoles
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A regioselective visible light induced synthesis of aryl α-thiocyano ketones/thiocyano alcohols from activated terminal aryl alkynes and aryl 1,3-conjugated dienes was achieved. This mild and non-metallic oxidation is exclusively driven by benign ambient air in the presence of an organic photo-catalyst and NH4SCN. This protocol was also demonstrated at the 5 mmol scale for the synthesis of potentially therapeutic 2-hydroxy 4-substituted arylthiazoles in good yields, signifying its amenability for large-scale application.
- Gullapalli, Kumaraswamy,Vijaykumar, Swargam
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p. 2232 - 2241
(2019/02/27)
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- Ammonium [11C]thiocyanate: revised preparation and reactivity studies of a versatile nucleophile for carbon-11 radiolabelling
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Herein we report the preparation of ammonium [11C]thiocyanate via the reaction of [11C]CS2 with ammonia. The [11C]SCN- ion is demonstrated as a potent nucleophile that can be used to readily generate a range of 11C-labelled thiocyanate molecules in high conversions. Furthermore, novel 11C-labelled thiazolone molecules can be easily prepared from the intermediate α-thiocyanatophenones via an acid mediated cyclisation reaction.
- Haywood, Tom,Cesarec, Sara,Kealey, Steven,Plisson, Christophe,Miller, Philip W.
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supporting information
p. 1311 - 1314
(2018/08/28)
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- Tetrazolinone compound and application for same
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Provided is a tetrazolinone compound given by formula (1) (wherein E represents the following group E16 or the like; Y represents -O-CH2- or the like; Q represents the following group Q46 or the like; R8 represents a C1-C6 alkyl group; R3, R30, and R31 may be the same or different, and represent hydrogen atoms or the like; A represents a C6-C16 aryl group or the like, optionally having one or more atoms or groups selected from the group P1; R5 represents a C1-C3 alkyl group; and X represents an oxygen or sulfur atom), and having exceptional efficacy in controlling harmful organisms.
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Paragraph 0690; 0691; 0692; 0693
(2016/10/08)
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- TETRAZOLINONE COMPOUNDS AND ITS USE
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The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein, R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, a C3-C12 cycloalkyl group or an adamantyl group, etc., which each optionally be substituted; R2 represents a hydrogen atom, an C1-C12 alkyl group, or a halogen atom, etc.; R4 and R5 represent independently of each other a hydrogen atom or an C1-C3 alkyl group, etc.; R6, R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, an C1-C12 alkyl group, a C1-C12 haloalkyl group, an C2-C12 alkenyl group, a C3-C12 cycloalkyl group, an C1-C12 alkoxy group or a C1-C12 haloalkoxy group, etc.; X and Y represent independently of each other a sulfur atom or an oxygen atom; Q represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.
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Paragraph 0465
(2013/11/18)
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- SUBSTITUTED THIAZOLE DERIVATIVES BEARING 3-PYRIDYL GROUPS, PROCESS FOR PREPARING THE SAME AND USE THEREOF
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The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.
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Page/Page column 40-41
(2008/06/13)
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- A correlative IR, MS, 1H, 13C and 15 NMR and theoretical study of 4-arylthiazol-2(3H)-ones
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Sixteen 4-arylthiazol-2(3H)-ones (3) were synthesised by cyclisation of α-thiocyanatoacetophenones (1) in acid solution. They appear to prefer greatly the oxo tautomeric forms. In CCI4 solution an equilibrium between the free C=O bond and a "di
- Pihlaja, Kalevi,Ovcharenko, Vladimir,Kolehmainen, Erkki,Laihia, Katri,Fabian, Walter M.F.,Dehne, Heinz,Perjessy, Alexander,Kleist, Marion,Teller, Joachim,Sustekova, Zora
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p. 329 - 336
(2007/10/03)
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- Hypervalent iodine in organic synthesis: One pot facile syntheses of α-thiocyanatoacetophenones, 2-hydroxy-, and 2-mercapto-4-arylthiazoles using [hydroxy (tosyloxy)iodo]benzene
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Hypervalent iodine oxidation of acetophenones (1a-1e) with [hydroxy(tosyloxy)iodo]benze, followed by treatment with potassium thiocyanate offers a new facile synthesis of corresponding α-thiocyanatoacetophenones (3a-3e). Cyclization of 3a-3e, thus generated in situ, using AcOH/H2O and H2NC(S)NH2/HCl provides one pot facile syntheses of 2-hydroxy-, and 2-mercapto-4-arylthiazoles (4 and 5) respectively.
- Prakash,Saini
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p. 1455 - 1462
(2007/10/02)
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