4-氟-2,1,3-苯并恶二唑 、 Chlorosulfate 、 在
氯仿 、 水 、 magnesium sulfate 作用下,
以
氯仿 为溶剂,
反应 3.0h,
以4.0 g of a pale brown needle-shaped crystalline substance with a melting point of between 64° and 66° C. were obtained的产率得到7-氟-2,1,3-苯并恶二唑-4-磺酰氯
参考文献:
名称:
Fluorogenic 2,1,3-benzoxadiazoles and fluorometric amine/thiol assays
Prodrugs of proton pump inhibitors of Formulas 1 through 4,
1
where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
Prodrugs of proton pump inhibitors background of the invention
申请人:Garst Michael
公开号:US20050143423A1
公开(公告)日:2005-06-30
Prodrugs of proton pump inhibitors of Formulas 1 through 4,
where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
The present invention provides a compound represented by the formula (I) and a salt thereof
wherein: ring A is a 5-membered aromatic heterocycle optionally having substituent(s); R
1
is a hydrogen atom or a hydrocarbon group optionally having substituent(s); W is an oxygen atom or a sulfur atom; X
1
and X
2
may be the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group, or, X
1
and X
2
in combination, optionally, form an oxygen atom, a sulfur atom or ═NR
2
; ring B is an aromatic ring optionally further having substituent(s); Y is a bond, C
1-6
alkylene C
2-6
alkenylene or C
2-6
alkynylene, optionally having substituent(s); and Z is —SO
n
R
3
or —COR
4
, which are useful as a pharmaceutical agent having GnRH antagonistic action.
Fluorogenic 2,1,3-benzoxadiazoles and fluorometric amine/thiol assays
申请人:Oread Laboratories, Inc.
公开号:US04769467A1
公开(公告)日:1988-09-06
Fluorogenic compounds are disclosed which are reactive with biologically important analytes including primary amines, secondary amines, and/or thiols and are of the general formula: ##STR1## wherein X is a group such as ##STR2## --CN, --CO.sub.2 CH.sub.3, or SO.sub.2 R, and wherein R is OR.sub.3, or Cl; R.sub.1 and R.sub.2 are hydrogen atoms or alkyl groups having 1 to 3 carbon atoms and R.sub.3 is a phenyl or benzyl group. The inventive compounds form a fluorescent adduct with the above analytes at the number 7 position of the benzoxadiazole ring. The fluorescent adduct thereby formed enables detection of very minute amounts of analyte (picomoles) using conventional fluorescent analytical methods.