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US 2002/0161220 A1Published application
Tetraphosphonate bicyclic trisanhydrides
AssigneePharmasset, Inc.
InventorsKrzysztof W. Pankiewicz, Krystyna Lesiak, Kyoichi A. Watanabe
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Abstract
Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.
Claims26
A compound having the following structure:
- 27
- wherein
- Z and Z1 are the same or different and are alkyl, aralkyl, aryl, aminoalkyl, alkyloxy, aralkyloxy, alkylamino, aralkylamino, arylamino, alkylmercaptan, aralkylmercaptan, arylmercaptan, carbohydrate, nucleoside, steroid, or substituted glyceride;
- and
- X is methylene (—CH2—), mono- or di-halo methylene, or —NR—, where R is H or alkyl.
2 more elements
A method for the preparation of a compound having the following structure:
- 28
- wherein
- Z and Z1 are the same or different and are alkyl, aralkyl, aryl, aminoalkyl, alkyloxy, aralkyloxy, alkylamino, aralkylamino, arylamino, alkylmercaptan, aralkylmercaptan, arylmercaptan, carbohydrate, nucleoside, steroid, or substituted glyceride;
- and
- X is methylene (—CH2—), mono- or di-halo methylene, or —NR—, where R is H or alkyl;
- which method comprises reacting a compound having the following structure:
- 29
- wherein Z and X are as described, with a dehydrating agent.
5 more elements
A method for the preparation of a compound having the following structure:
- 30
- wherein
- Z and Z1 are the same or different and are alkyl, aralkyl, aryl, aminoalkyl, alkyloxy, aralkyloxy, alkylamino, aralkylamino, arylamino, alkylmercaptan, aralkylmercaptan, arylmercaptan, carbohydrate, nucleoside, steroid, or substituted glyceride;
- and
- X is methylene (—CH2—), mono- or di-halo methylene, or —NR—, where R is H or alkyl;
- which method comprises reacting a compound having the following structure:
- 31
- wherein Z, Z1 and X are as defined above, with a dehydrating agent.
5 more elements
A method for the preparation of a compound having the following structure:
- 32
- wherein
- Z and Z1 are the same or different and are alkyl, aralkyl, aryl, aminoalkyl, alkyloxy, aralkyloxy, alkylamino, aralkylamino, arylamino, alkylmercaptan, aralkylmercaptan, arylmercaptan, carbohydrate, nucleoside, steroid, or substituted glyceride;
- and
- X is methylene (—CH2—), mono- or di-halo methylene, or —NR—, where R is H or alkyl;
- which method comprises reacting a compound having the following structure:
- 33
- wherein Z, Z1 and X are as defined above, with a nucleophilic agent.
5 more elements
A compound having the following structure:
- 34
- wherein
- Z and Z1 are the same or different and are alkyl, aralkyl, aryl, aminoalkyl, alkyloxy, aralkyloxy, alkylamino, aralkylamino, arylamino, alkylmercaptan, aralkylmercaptan, arylmercaptan, carbohydrate, nucleoside, steroid, or substituted glyceride;
- and
- X is methylene (—CH2—), mono- or di-halo methylene, or —NR—, where R is H or alkyl.
2 more elements
A compound having the following structure:
- 35
- wherein
- each of R1, R2, R3, and R4 is independently H, OH or F;
- X is O, S, mono- or di-halomethylene, or NR wherein R is H or alkyl, or CH2;
- Y is OH, SH or F;
- and
- each of W1 and W2 is independently H, OH, ═O, OR, SH, SR, NH2, NHR or NR2, wherein R is C1-C5 alkyl and n is an integer from 1 to 5.
4 more elements
Dependencies are inferred from the claim text.