Method of forming methyl penam derivatives
AssigneeAllecra Therapeutics SAS
InventorsAndrea Faini, Marco Forzatti, Giovanni Fogliato, Stefano Biondi
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Abstract
A method of forming a compound of formula (IIIa): wherein: R1 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C1-5 alkenyl and C1-5 alkynyl; R2 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C1-5 alkenyl and C1-5 alkynyl; R4 is C1-5 alkyl; and R6 is a C1-5 fluoroalkyl; and PG is a protecting group, the method comprising the step of reacting a compound of formula (IIa) with a compound of formula (VIII):
Claims19
A method of forming a compound of formula (IIIa):
- wherein:
- R1 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C2-5 alkenyl and C2-5 alkynyl;
- R2 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C2-5 alkenyl and C2-5 alkynyl;
- R4 is C1-5 alkyl;
- and
- R6 is a C1-5 fluoroalkyl;
- and
- PG is a protecting group,
- the method comprising the step of reacting a compound of formula (IIa) with a compound of formula (VIII):
A method of forming a compound of formula (IV):
- wherein R1 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C2-5 alkenyl and C2-5 alkynyl;
- R2 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C2-5 alkenyl and C2-5 alkynyl;
- and R4 is C1-5 alkyl;
- the method comprising the step of reacting a compound of formula (III) with a 2-ethylhexanoate salt:
- wherein X— is an anion and each R3 is independently selected from the group consisting of C1-10 hydrocarbyl and C1-5 alkoxy.
A method of forming a compound of formula (II)
- wherein R1 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C2-5 alkenyl and C2-5 alkynyl;
- R2 in each occurrence is independently selected from H, halogen, amino, C1-5 alkyl, C2-5 alkenyl and C2-5 alkynyl;
- and R3 in each occurrence is independently selected from the group consisting of C1-5 alkoxy and C1-10 hydrocarbyl;
- the method comprising the step of reacting a compound of formula (I) with less than a molar equivalent of a compound of formula (V)
- wherein R5 is C1-5 alkyl.
Dependencies are inferred from the claim text.