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1. WO2009004639 - A DENDRITIC MACROMOLECULE AND A PROCESS THEREOF

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[ EN ]AMENDEDinitial

AMENDED CLAIMS
received by the International Bureau on 16 October 2008 (16.10.08);
claims 1-12 replaced by amended claims 1-13

1, A dendritic macromolecule, wherein the branch points are tertlary amines, the branches linked together through linkers comprising oxygen atom of an ether, and the heteroatoms are separated by a substituted or non-substituted linear three methylene linker, wherein the said dendritic macromolecule has four or more

2. A dendritic macromolecule of claim 1, where the number of functional groups at the surfrce being equal to 16 to at least n - (4X 2y ), where "n" is number of functional groups at surface of a dendrimer generation, "X" is symbol for multiplication and "y" is the generation number of the immediate previous generation. The functional groups on the surface being uniformly of one of alcohol, nitrile, primary amine, ester, oarboxyl or a mixture of any two or more; accordingly a number of functional groups at the surface being at least equal to 16 for third generation, 32 for fourth generation, 64 for fifth generation, 128 for sixth generation, 256 for seventh generation, 512 for eighth generation and the like.
3. The dendritic macromolecule as claimed in claim 1, wherein the number of symmetrically sited branches, are ranging from 3 to 8 and the number of peripheral groups ranging from 16 to at least 512.
4. The dendritic macromolecule as claimed in claim 1, wherein the substltuents on the three methylene linkers are selected from a group comprising an alkyl, b h d lk l and ayl g oup

6. The dendritic macromolecule as claimed in claim 1, wherein repeating unit of the dendritic nmcrornolecule is;




R4 = H, alKyl, ary!
7. A process for preparing a dendritic macromolecule having substantially symmetrically sited branches, wherein the branch points are tertiary amines, the branches linked together through linkers comprising oxygen atom of an ether, and the heteroatoms are separated by a substituted or non-substituted linear three methylene linker, wherein the said dendritic macromolecule had four or more generations of dendrons, comprising reiterative steps of:

a, reacting the alcohol units of isolated pure lower dendritic molecule to react with molar equivalents of α,β-unsaturated nitrile, in the presence of an alkali, to install nitrile groups at the surfaces of the dendritic macromolecule, wherein (i) at least about 4 molar equivalents or more of nitrile units were required per unit of the hydroxy! group, (ii) the reagent containing nitrile was added in more than one lots at time intervals, (iii) the reaction was carried out for more than six hours, (iv) the product having nitrile groups on surface was isolated from the by-products in pure form and then subjected to next step of reaction;

b. converting nitrile groups at the surfaces of the dendritic macromolecule to the corresponding amines, mediated by supported metal catalysts and hydrogen gas; wherein (i) the concentration of the nitrile compound in water is between 0.01-4.0 mM, more preferably between 04-0.4 mM and (ii) the weight ratio of the nitrile compound to the supported metal catalyst is generally 1:15 and, most preferably in the range of 1;3 to 1:7, (iii) heated for at least around 3.5 hour, and (iv) the product of the reaction was isolated in pure form and then subjecting to next reiterative reaction;

c. subjecting the resulting amine functional groups to react with α,β- unsaturated esters; wherein the ratio of ester units to eadh unit of amine functionalities present at the surfaces of the dendritio macromolecule required for satisfactory conversion is in excess of 3.33:1 up to 200:1, most preferable ratio is In the range of 5-60 molar equivalent of tert-butyl acrylate per one unit of amine present at the surfaces, the product of the reaction was isolated in pure form and then subjecting to next reiterative reaction, and
d. converting ester units present at the surfaces of the dendritic macromolecule to the corresponding alcohol units, mediated by metal hydride reagents; to prepare a higher generation dendritic molecule, wherein the molar ratio of metal hydride generally is 0.5 to 4 per one ester unit, the preferable molar ratio of the metal hydride is 2 per unit of ester , methanol is added to wash the compound from catalyst and to remove the catalyst torn pellet picker, flushed with water, dioxane added to the water layer and azeotrσp of water removed by concentrating at 55 °C under reduced pressure, adding methanol to the resulting reaction mixture followed by filtration and the product is isolated from reaction mixture in pure form for subjecting the same to next cycle of reiterative reactions.

8. A process of claim 7 wherein:

a. the said alkali used is 40% aqueous solution of sodium hydroxide, the said b. the said the supported metal catalyst is selected from a group of metal supported catalysts such as Raney alloys; preferably Raney Cobalt;
c. the said metal hydride reagent is selected from a range of metal hydride reagents preferably lithium aluminum hydride,
9. The process of claim 7 wherein isolation and purification of the end product of every reiterative reaction may be done on the basis of differential solubility, wherein the byproducts arising after the work-up of the reaction, are removed by: (i) washing the crude product with water; (ii) filtration; (iii) removal of water under reduced pressure; (iv) washing the product with MeOH: (v) filtration; (vi) removal of MeOH under reduced pressure and (vii) extraction of the product with CHCl3 and removal of the solvents under reduced pressure, and (viii) repeating the reaction to eliminate any inorganic byproducts, if required,
10. The process as claimed in claim 7, wherein the lower dendritic molecule is one generation lower than the target dendritic molecule.
11. A composition of matter containing dendritic macromolecule of claim 1 as an ingredient and one or more of an other active ingredients.
12. A composition of claim 11 wherein the said other ingredient is one or more of a fragrance, drug, antibodies, antigens, nucleotide, nucleoside, carbohydrate, peptide, protein, biocide, lubricant and the like.
13. A dendritic molecule, a process of its preparation, and compositions containing the dendritic molecules substantially as herein described with reference to foregoing examples and drawings,