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Details for Patent: 4,987,223

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Details for Patent: 4,987,223

Title: Derivatives of the uronic acid
Abstract:The invention relates to derivatives with a uronic acid structure having substituents selected among a reactive group, a functionalisable group and --OH functions blocked by protective groups. These derivatives are useful for preparing glycosides, particularly enzyme substrates.
Inventor(s): Choay; Jean (Paris, FR), Jacquinet; Jean-Claude (Orleans-La-Source, FR), Petitou; Maurice (Paris, FR), Sinay; Pierre (Orleans, FR)
Assignee: Choay S.A. (Paris, FR)
Filing Date:Oct 27, 1982
Application Number:06/453,731
Claims:1. A compound having the following formula: ##STR10## wherein a. R.sub.1 is selected from group consisting of

i. Br,

ii. Cl,

iii. --O-- imidoyl,

iv. --O-allyl,

v. --O-vinyl,

vi. --OCH.sub.3,

vii. --O--C.sub.6 H.sub.5,

viii. --O--CO--CH.sub.3,

Xi. --OH,

x. an orthoester which together with --OR.sub.2 forms --OH(CH.sub.3)OtBu)O--,

xi. an orthoester which together with --OR.sub.2 forms --OC(CH.sub.3)(OCH.sub.3)O--, and

xii. --O-nitrophenyl;

b. R.sub.2 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl,

vii. vinyl,

viii. an orthoester which together with --OR.sub.1 forms --OC(CH.sub.3)(OtBu)O--, and

ix. an orthoester which together with --OR.sub.1 forms--OC(CH.sub.3)(OCH.sub.3)O--;

c. R.sub.3 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl, and

vii. vinyl;

d. R.sub.4 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl,

vii. vinyl, and

viii. paramethoxy benzyl;

e. R.sub.6 is selected from the group consisting of

i. methyl,

ii. benzoyl, and

iii. a cation of a pharmaceutically acceptable salt;

provided that

where R.sub.1 is a methoxy group, R.sub.4 is not methyl,

where COOR.sub.6 is in the glucuronic position, R.sub.2, R.sub.3, and R.sub.4 are not identical,

where R.sub.1 and R.sub.2 form an orthoester, R.sub.3 and R.sub.4 are not acetyl,

at least one of R.sub.2 or R.sub.3 is acetyl.

2. A compound having the following formula: ##STR11## wherein a. R.sub.1 is selected from group consisting of

i. --O-allyl,

ii. --O-vinyl, and

iii. --OH;

b. R.sub.2 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyle,

vi. allyl,

vii. vinyl,

viii. or orthoester which together with --OR.sub.1 forms --OC(CH.sub.3)(OtBu)O--, and

ix. an orthoester which together with --OR.sub.1 forms --OC(CH.sub.3 (OCH.sub.3)O--;

c. R.sub.3 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl, and

vii. vinyl;

d. R.sub.4 is selected from the group consisting of

i. monochloroacetyl,

ii. acetyl,

iii. benzyl,

vi. p-methoxybenzyl,

v. allyl, and

vi. vinyl;

e. R.sub.6 is selected from the group consisting of

i. methyl,

ii. benzyl, and

iii. a cation of a pharmaceutically acceptable salt;

provided that

where COOR.sub.6 is in the glucuronic position, R.sub.2, R.sub.3, and R.sub.4 are not identical

where R.sub.1 and R.sub.2 form an orthoester, R.sub.3 and R.sub.4 are not acetyl.

3. A compound having the following formula: ##STR12## wherein a. R.sub.1 is --OH;

b. R.sub.2 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl,

vii. vinyl,

viii. an orthoester which together with --OR.sub.1 forms --OC(CH.sub.3)(OtBu)O--, and

ix. an orthoester which together with --OR.sub.1 forms --OC(CH.sub.3)(OCH.sub.3)O--;

c. R.sub.3 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl, and

vii. vinyl;

d. R.sub.4 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl,

vii. vinyl, and

viii. paramethoxy benzyl;

e. R.sub.6 is selected from the group consisting of

i. methyl,

ii. benzyl, and

iii. a cation of a pharmaceutically acceptable salt;

provided that

where COOR.sub.6 is in the glucuronic position, R.sub.2, R.sub.3, and R.sub.4 are not identical.

4. A compound according to claim 1, wherein R.sub.1 is --OH.

5. A compound having the following formula ##STR13## wherein a. R.sub.1 is --O-allyl;

b. R.sub.2 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl,

vii. vinyl,

viii. an orthoester which together with --OR.sub.1 forms --OC(CH.sub.3)(OtBu)O--, and

ix. an orthoester which together with --OR.sub.1 forms --OC(CH.sub.3)(OCH.sub.3)O--;

c. R.sub.3 is selected from the group consisting of

i. methyl,

ii. benzyl,

iii. acetyl,

iv. benzoyl,

v. chloroacetyl,

vi. allyl, and

vii. vinyl;

d. R.sub.4 is --OH;

e. R.sub.6 is selected from the group consisting of

i. methyl,

ii. benzyl, and

iii. a cation of a pharmaceutically acceptable salt.

6. A compound according to claim 1, wherein R.sub.4 is --OH, and R.sub.1 is --O-allyl.
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