Supports useful in solid phase synthesis of oligonucleotides

Claim 2

A support of the formula ##STR36## wherein ○P is micropellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene of 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x is an integer from 0 to 20, x 1 is an integer from 0 to 10 and the amino group may be in the m-, p- or o-position.

Claim 3

A support of claim 1 wherein ○P is a silica material having a homogeneous particle size and the amine groups on the phenyl are in the meta- or para-position.

Claim 4

A support of claim 1 wherein m is an integer from 1 to 5.

Claim 5

A support of claim 1 wherein A is --CH 2 --.

Claim 6

A support of claim 1 wherein x is an integer from 0 to 10 and x 1 is an integer from 0 to 5.

Claim 7

A support of claim 1 wherein m is 3.

Claim 8

A support of claim 1 selected from the group consisting of ##STR37## wherein Si is Vydac A silica.

Claim 9

A process for the preparation of a support of claim 1 comprising reacting a support of the formula ##STR38## wherein ○P and m have the above definitions with a compound of the formula ##STR39## wherein R is a protective group for a mono- or divalent amine and A and x 1 have the above definitions in the presence of an activating agent and a tertiary base to obtain a support of the formula ##STR40## reacting the latter, depending on the nature of R, with an acid or a base to free the terminal --NH 2 -- to obtain a support of formula I in which ○P , m, A and x 1 have the above definitions and x=0, and optionally reacting the latter with the compound of formula III under the same conditions as before to obtain an intermediate support of the formula ##STR41## which intermediate is reacted again with an acid or a base to obtain a support of formula I in which x=1, and optionally repeating the procedure successively in this fashion passing via intermediate supports of the formula ##STR42## wherein R, ○P , m and x 1 have the above definitions and x is an integer from 0 to 20 until a support of formula I wherein x is 20 is obtained.

Claim 10

The process of claim 8 wherein R is ##STR43##

Claim 11

An intermediate support of the formula ##STR44## wherein ○P is micro pellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x 1 is an integer from 0 to 10 and R is a protective group for a mono-or divalent amine.

Claim 12

An intermediate support of the formula ##STR44## wherein ○P is micro pellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x 1 is an integer from 0 to 10 and R is a protective group for a mono-or divalent amine.