15601-88-4Relevant articles and documents
Synthesis method of drug for treating diabetes
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, (2018/06/23)
The invention relates to the fields of organic synthesis and pharmacy, and particularly relates to a synthesis method of a drug for treating diabetes. The synthesis method comprises the following steps of (1), hydrolyzing 2-cyanophenyl tert-butyl sulfide to produce o-carbamoylphenyl tert-butyl sulfide; (2), oxidizing the o-carbamoylphenyl tert-butyl sulfide to produce o-carbamoylphenyl tert-butylsulfoxide; (3), enabling the o-carbamoylphenyl tert-butyl sulfoxide to generate an intramolecular multicomponent reaction with phenyl isocyanide to produce 2-(aniline)-4H-benzo[e][1,3]thiazin-4-one. The synthesis method is simple, convenient and environmentally friendly, is easy to operate and suitable for industrialized production, and is low in cost and high in yield; synthesis raw materials areeasily obtained, and the atom economy is achieved.
Thermolysis-Induced Two- or Multicomponent Tandem Reactions Involving Isocyanides and Sulfenic-Acid-Generating Sulfoxides: Access to Diverse Sulfur-Containing Functional Scaffolds
Wu, Shengfeng,Lei, Xiaofang,Fan, Erkang,Sun, Zhihua
supporting information, p. 522 - 525 (2018/02/10)
Direct reaction of isocyanides with some sulfenic-acid-generating sulfoxides led to the effective formation of the corresponding thiocarbamic acid S-esters in good to high yields. A multicomponent reaction involving isocyanide, sulfoxide, and a suitable nucleophile has also been developed, providing ready access to a diverse range of sulfur-containing compounds, including isothioureas, carbonimidothioic acid esters, and carboximidothioic acid esters.
Alkylation of 1,3-benzothiazin-4-one 2-oxo-, 2-arylimino-, and 2-thioxo derivatives
Shestakov, Alexandr S.,Prezent, Mikhail A.,Zlatoustovskaya, Evgenia O.,Shikhaliev, Khidmet S.,Falaleev, Alexandr V.,Sidorenko, Oleg E.
, p. 370 - 376 (2016/01/12)
[Figure not available: see fulltext.] Sodium salt of 3H -benzo[e][1,3]thiazine-2,4-dione is easily alkylated at position 3. In the case of 2-(arylimino)-2,3-dihydrobenzo[e][1,3]-thiazin-4-ones, the alkylation reaction at this position occurs regioselectively. Alkylation of 2-thioxo-2,3-dihydrobenzo[e][1,3]thiazin-4-one under the same conditions produced regioisomers, but S-alkylation at the exocyclic sulfur atom occurred in the presence of triethylamine. The reaction of 1-(4-oxo-3,4-dihydrobenzo[e][1,3]thiazin-2-ylidene)guanidine with methyl anthranilate led to the formation of tetracyclic quinazolino[2,1-b]quinazolinedione.
HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 -HYDROXYSTEROID DEHYDROGENASE
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Page/Page column 31-32, (2010/08/07)
Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
Novel Construction of 4H-2,3-Dihydro-1,3-benzothiazine Ring via Nickel(0)-Catalyzed Reaction of o-Iodobenzamide or o-Iodobenzonitrile with Thioureas
Takagi, Kentaro
, p. 2205 - 2206 (2007/10/02)
Nickel(0) complex induced the catalytic reaction of o-iodobenzamide or o-iodobenzonitrile with thioureas giving rise to cyclized products, 4H-2,3-dihydro-2-imino-1,3-benzothiazin-4-one or 4H-2,3-dihydro-1,3-benzothiazine-2,4-diimine.
