Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form

A technology of reagents and dosage forms, applied in the quantitative field of solid reagents

Inactive Publication Date: 2003-07-09
H LUNDBECK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In general, tablets of these known kinds are not suitable as dosing forms in parallel syntheses, since they introduce, besides the required reagents, various auxiliaries etc., whose presence in the synthesis medium is unacceptable and difficult to extract from which removed

Method used

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  • Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form
  • Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form

Examples

Experimental program
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Effect test

Embodiment 1

[0119] Example 1. Mitsunobu reaction using tablets comprising polystyrene, di-tert-butylazodicarboxylate and diphenylphosphorylpolystyrene with tablets of isocyanatomethylpolystyrene

[0120] The evaluation results are summarized in Table 3. A detailed description of the steps described follows:

[0121]2-(2-Phenylthio-ethyl)-2H-naphtho[1,8-cd]isothiazole 1,1-dioxide (entry 1). Tablets containing a total of 0.22 mmol di-tert-butylazodicarboxylate and 0.29 mmol resin-bound diphenylphosphine were added with 2H-naphtho[1,8-cd]isothiazole 1,1- Solution of dioxide (21.0 mg, 0.10 mmol) and 2-phenylthio-ethanol (29.9 mg, 0.20 mmol) in THF (3 mL). After stirring for 16 h, THF (2 mL) and a tablet containing isocyanatomethylpolystyrene (150 mg, 0.15 mmol) were added. The mixture was stirred at 60 °C for 2 h. The resin was filtered and washed with dichloromethane (1 x 1 mL), methanol (1 x 1 mL) and dichloromethane (1 x 2 mL). Trifluoroacetic acid (0.4 mL) was added to the combined f...

Embodiment 2

[0129] Example 2. Acylation reaction using tablets comprising polystyrene, tetrabromomethane and diphenylphosphorylpolystyrene with tablets of isocyanatomethylpolystyrene

[0130] The evaluation results are summarized in Table 4. A detailed description of the steps described follows:

[0131] 4-Morpholinocarbonylferrocene (entry 6). To a tablet containing 0.11 mmol tetrabromomethane and 0.15 mmol resin-bound diphenylphosphine was added ferrocenecarboxylic acid (23.3 mg, 0.10 mmol), morpholine (10.7 mg, 0.12 mmol) and triethylamine at 0 °C (22.6 mg, 0.22 mmol) in dry THF (1.5 mL). After stirring at room temperature for 16 h, THF (2 mL) and a tablet (150 mg) containing isocyanatomethylpolystyrene (0.15 mmol) were added. The mixture was stirred at 60 °C for 2 h. The resin was filtered and washed with dichloromethane (1 x 1 mL), methanol (1 x 1 mL) and dichloromethane (1 x 2 mL). The solvent was evaporated in vacuo and the residue was purified by solid phase extraction (hepta...

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Abstract

A dosing form for at least one solid reagent for use in conventional organic and inorganic synthesis, in parallel synthesis, and in split and mix synthesis in combinatorial chemistry is provided as compressed tablets each containing the same predetermined amount of said at least one reagent embedded in a polymer matrix comprising beads of a polymer insoluble in the solvents for the intended synthesis, which tablets are capable of disintegrating in said solvent for release of the at least one reagent and disperse the matrix as polymer beads into the solvent. The polymer beads forming the matrix and the reagents of the dosing form can easily be removed by filtration in order to separate these from a formed soluble product. In a method for producing the dosing form, beads of one or more polymers are mixed with the reagents and compressed into tablets after pre-treatment with an aprotic organic solvent.

Description

field of invention [0001] The present invention relates to the quantification of solid reagents in the field of organic and inorganic chemistry. In particular, the present invention relates to such dosing forms for use in parallel syntheses or mixed and split syntheses in the field of organic chemistry, such as combinatorial and medicinal chemistry. Background of the invention [0002] Synthetic and analytical chemistry involves numerous process steps involving the addition of chemicals, especially in parallel or mixing and splitting syntheses in the fields of organic chemistry such as combinatorial and medicinal chemistry. [0003] Parallel synthesis has become an important method in the search for new compounds in eg the pharmaceutical industry and materials science. Using these concepts, a large number of compounds have been synthesized. Parallel synthesis is a particular approach for histochemical synthesis in which many chemical syntheses are performed simultaneously ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01J4/02B01J19/00C07B61/00C07D295/12C07C231/02C07C233/05C07C235/56C07C319/20C07C323/12C07D209/48C07D213/75C07D233/60C07D275/06C07D295/16C07D453/02C07K1/02C07K1/04C07K1/107C08K5/00C08L25/04C08L71/02C08L101/00C40B40/04C40B50/00C40B60/14
CPCC07K1/023B01J2219/0059C07K1/1077B01J2219/00459B01J2219/00585B01J2219/005B01J2219/00497B01J19/0046B01J2219/00351B01J2219/00592C07K1/04B01J4/02C40B60/14B01J19/00
Inventor T·鲁兰德P·霍尔姆K·舒尔茨J·埃格斯科夫霍尔姆K·安德森
Owner H LUNDBECK AS
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