90814-91-8Relevant academic research and scientific papers
Facile synthesis of 1,4-benzothiazin-3-ones from Cu-catalyzed coupling of 2-iodoanilines and 2-mercaptoacetate
Huang, Wei-Sheng,Xu, Rongsong,Dodd, Rory,Shakespeare, William C.
, p. 5214 - 5216 (2013/09/02)
A novel synthesis of 1,4-benzothiazin-3-ones was developed from Cu-catalyzed coupling of readily available substituted 2-iodoanilines with 2-mercaptoacetate. The new method offers clear advantages over existing approaches for its one-step simple operation, wider reaction scope, and moderate to excellent isolated yields.
SUBSTITUTED 2-BENZYLIDENE-2H-BENZO[b][1,4]THIAZIN-3(4H)-ONES, DERIVATIVES THEREOF, AND THERAPEUTIC USES THEREOF
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Page/Page column 74-75, (2013/02/28)
The present invention relates to compounds according to Formula I and salts thereof, wherein R1, R2, R3, R4, Ar, and n are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
The bromination and nitration of some (2H)-1,4-benzoxazin-3(4H)-ones
Hanson, James R.,Richards, Lisa,Rozas, Panteleimon
, p. 1120 - 1128 (2007/10/03)
Bromination of (2H)-1,4-benzoxazin-3-(4H)-one with bromine in glacial acetic acid gave firstly the 6-bromo and then the 6,7-dibromo compound whilst bromine in chloroform gave mainly the 7-bromo derivative. Bromination of the 6-chloro- and 6-methyl-(2H)-1,4-benzoxazin-3(4H)-ones and (2H)=1,4-benzothiazin-3(4H)-one gave the 7-bromo compounds. Nitration of (2H)-1,4-benzoxazin-3(4H)-one with a sulfuric acid : nitric acid mixture gave the 6-nitro and then 6,8-dinitro compound whilst nitrosation: nitration with sodium nitrite : fuming nitric acid gave mainly the 7-nitro compound. 6-Chloro-(2H)-1,4-benzoxazin-3(4H)-one gave 7-nitro compound.
Benzimidazolones and analogues
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, (2008/06/13)
The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5are independently selected from H or optionally substituted C1to C6alkyl, C2to C6alkenyl, C2to C6alknyl, C3to C8cycloalkyl, substituted C3to C8cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4and R5to from a 5 to 7 membered ring; R1is selected from H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, substituted C1to C6alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1to C3alkyl), —CO(aryl), —CO(C1to C3alkoxy), or —CO(C1to C3aminoalkyl) groups; R2is selected from H, halogen, CN, NO2, or optionally substituted C1to C6alkyl, C1to C6alkoxy, or C1to C6aminoalkyl groups; R3is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.
Combination therapies using benzimidazolones
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, (2008/06/13)
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R6are independently selected from H or optionally substituted C1to C6alkyl, C2to C6alkenyl, C2to C6alkynyl, C3to C8cycloalkyl, substituted C3to C8cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4and R5to from a 5 to 7 membered ring; R1is selected from H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, substituted C1to C6alkenyl, alkynyl, substituted alkynyl, —COH, or optionally substituted —CO(C1to C3alkyl), —CO(aryl), —CO(C1to C3alkoxy), or —CO(C1to C3aminoalkyl) groups; R2is selected from H, halogen, CN, NO2, or optionally substituted C1to C6alkyl C1to C6alkoxy, or C1to C6aminoalkyl groups; R3is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromnatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate. These combinations may also be used to in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.
3-H-1,2,3-Benzodithiazole-2-oxides as synthons for the synthesis of five- and six-membered heterocycles containing sulphur and nitrogen
Sawhney, S N,Sharma, P. K.,Bajaj, K,Gupta, A
, p. 280 - 284 (2007/10/02)
The reaction of 6-substituted-1,2,3-benzodithiazole-2-oxides (2) with aromatic aldehydes, carboxylic acids and acid chlorides in the presence of an organic base such as triethylamine and N,N-dimethylaniline lead to the formation of 6-substituted-2-arylben
