Peter J Bonk

US Patent:

7700614, Apr 20, 2010

Filed:

Dec 14, 2005

Appl. No.:

11/300671

Inventors:

Madhup K. Dhaon - Mundelein IL, US
Chi-nung Hsiao - Taipei County, TW
Subhash R. Patel - Chicago IL, US
Peter J. Bonk - Westerly RI, US
Sanjay R. Chemburkar - Gurnee IL, US
Yong Chen - Lake Villa IL, US

Assignee:

Abbott Laboratories - Abbott Park IL

International Classification:

C07D 498/18

US Classification:

514291, 540456

Abstract:

A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at −30 C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane.

US Patent:

8129521, Mar 6, 2012

Filed:

Feb 23, 2010

Appl. No.:

12/711072

Inventors:

Madhup K. Dhaon - Mundelein IL, US
Chi-nung Hsiao - Taipei County, TW
Subhash R. Patel - Chicago IL, US
Peter J. Bonk - Westerly RI, US
Sanjay R. Chemburkar - Gurnee IL, US
Yong Y. Chen - Lake Villa IL, US

Assignee:

Abbott Laboratories - Abbott Park IL

International Classification:

C07D 498/18

US Classification:

540456

Abstract:

A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at −30 C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane.

US Patent:

56774630, Oct 14, 1997

Filed:

Nov 20, 1996

Appl. No.:

8/754772

Inventors:

Peter J. Bonk - Kenosha WI

Assignee:

Abbott Laboratories - Abbott Park IL

International Classification:

C07D26336

US Classification:

548225

Abstract:

The present invention relates to the production of pemoline and its intermediates.