US 6,982,315 B2 | ||
Process for the preparation of carboxamides | ||
Joachim Rudolph, Guilford, Conn. (US); Günther Jung, Tubingen (Germany); and Bernd Thern, Tubingen (Germany) | ||
Assigned to Bayer Aktiengesellschaft, Leverkusen (Germany) | ||
Filed on Mar. 27, 2002, as Appl. No. 10/108,667. | ||
Claims priority of application No. 101 15 213 (DE), filed on Mar. 28, 2001; application No. 101 26 431 (DE), filed on May 31, 2001; and application No. 101 57 882 (DE), filed on Nov. 26, 2001. | ||
Prior Publication US 2002/0193594 A1, Dec. 19, 2002 | ||
Int. Cl. C07K 1/00 (2006.01); C07K 1/02 (2006.01); C07K 1/04 (2006.01); C07K 1/10 (2006.01) |
U.S. Cl. 530—333 | 26 Claims |
1. A process for the preparation of carboxamides from an acid component in the form of a compound having at least one carboxyl
groups and an amine component in the form of a compound having at least one primary or secondary amino group, comprising the
following steps:
i) introducing the amine component into a solvent together with a coupling base in the form of a sterically hindered trialkyl
amine,
ii) adding the acid component to a solvent with an activating reagent in the form of a carbonate of the formula I,
O═C(—OX)2 (I)
which contains the two identical or different electron-withdrawing groups X which are separate or connected to one another,
or its monohalide of the formula II,
O═C(—OX)Y (II)
in which X has the same meaning as in formula I and Y represents a halogen atom,
or its dihalide of the formula III,
O═CYY′ (III)
in which Y and Y′ independently of one another each represent a halogen atom,
and an activating base in the form of a sterically hindered momo- or polyalkyl-substituted pyridine and
(iii) adding the mixture containing the acid component as in (ii) to the mixture containing the amino component as in (i).
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