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AssigneeCyclacel Pharmaceuticals Inc.
InventorsBenjamin SKEAD, Derek LONDESBROUGH, Michal CZYZEWSKI, Chris ATHERTON, Chris GILL, Alex HUDSON
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In one aspect, the invention relates to a process for preparing a compound of formula (XII), wherein PG is a protecting group, or a compound of formula (XI), comprising the steps of: (i) treating a compound of formula XIII, wherein PG is a protecting group, with N-methylpiperazine to form a compound of formula XII, wherein said compound of formula XII is in the form of a mixture of cis and trans isomers; (ii) combining the mixture formed in step (i) with an organic solvent and heating the solvent mixture so formed; (iii) isolating the trans-isomer of the compound of formula XII from the solvent mixture formed in step (ii); and (iv) optionally treating said trans-isomer of the compound of formula XII with an acid to form a compound of formula XI; and isolating said compound of formula XI. Further aspects of the invention relate to processes for preparing pyrimido-diazepinone derivatives using the above process and intermediates.
A process for preparing a compound of formula (XII), wherein PG is a protecting group, or a compound of formula (XI), comprising the steps of:
A process according to any preceding claim wherein step (i) comprises the steps of:
A process according to any preceding claim wherein the organic solvent in step (ii) is acetonitrile.
A process according to any preceding claim wherein step (ii) comprises heating the solvent mixture.
A process according to any preceding claim wherein step (iii) comprises cooling the mixture such that the compound of formula XII precipitates out of solution, filtering the precipitate so formed, and optionally washing and/or drying the precipitate.
A process according to any preceding claim wherein step (iii) comprises cooling the mixture to a temperature of from 0 to about 15° C., more preferably, from about 5 to about 10° C.
A process according to any preceding claim wherein the compound of formula XII obtained in step (iii) is substantially free from the cis-isomer.
A process according to any preceding claim which comprises the step of treating said compound of formula XII with an acid to form a compound of formula XI.
A process of preparing a compound of formula I, or a pharmaceutically acceptable salt thereof, which comprises the steps of:
A process for preparing a compound of formula II comprising the steps of contacting a compound of formula III with a compound of formula X in N-methylpyrrolidone, and isolating the compound of formula II:
Dependencies are inferred from the claim text.