The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 08, 2001
Filed:
Apr. 07, 1999
Applicant:
Inventors:
Carolina L. Lanter, Hillsborough, NJ (US);
Joseph W. Guiles, Bedminster, NJ (US);
Ralph A. Rivero, North Wales, PA (US);
Assignee:
Ortho-McNeil Pharmaceutical, Inc., Raritan, NJ (US);
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 3/812 ; C07K 5/00 ; C07K 1/600 ; C07K 1/700 ; G01N 3/3543 ;
U.S. Cl.
CPC ...
A61K 3/812 ; C07K 5/00 ; C07K 1/600 ; C07K 1/700 ; G01N 3/3543 ;
Abstract
The preparation of 14-membered macrocycles from a resin-bound orthogonally protected lysine residue is described. Reductive alkylation of the a-nitrogen followed by acylation with an Fmoc-aminoacid provides a protected dipeptide precursor. Removal of the Fmoc-group, acylation with a succinic anhydride, methyltrityl-group removal and macrocyclization provides the desired macrocycles, after TFA cleavage, in excellent yield and purity.