Novel aspartame derivative crystal and process for producing...

Details Novel aspartame derivative crystal and process for producing... Novel aspartame derivative crystal and process for producing...

C - Chemistry, Metallurgy

07

K

C07K 5/075 (2006.01) C07K 1/02 (2006.01) C07K 5/072 (2006.01)

Patent

CA 2331810

A process for producing crystals of a methyl ester of N-[N-(3,3-dimethylbutyl)- L-.alpha.-aspartyl]-L-phenylalanine which comprises precipitating the ester from an aqueous solution thereof at a crystallization temperature of 25 ~C or lower, further cooling the solution if desired, subsequently separating the precipitated crystals (B-form crystals) by solid-liquid separation, and then drying the crystals. The thus-dried crystals are novel crystals (D-form crystals) of the ester which have an excellent rate of dissolution. These crystals, when examined by X-ray powder diffractometry, have characteristic X- ray diffraction peaks at least at diffraction angles of 5.4~, 8.4~, 18.8~, and 17.6~ (2.theta., CuK.alpha. line).

L'invention concerne un procédé permettant de produire des cristaux d'un éther méthylique de N-[N-(3,3-diméthylbutyl)-L-.alpha.-aspartyl]-L-phénylalanine, consistant à faire précipiter l'éther à partir d'une solution aqueuse de celui-ci, à une température de cristallisation de 25 ·C ou inférieure, à refroidir ladite solution le cas échéant, à séparer les cristaux précipités (cristaux de forme B) par séparation solide-liquide, et à sécher lesdits cristaux. Les cristaux ainsi séchés sont de nouveaux cristaux (cristaux de forme B) de l'éther présentant une excellente vitesse de dissolution. Ces cristaux, lorsqu'on les examine par diffraction aux rayons X, présentent des pics de diffraction aux rayons X caractéristiques, au moins à des angles de diffraction de 5,4·, 8,4·, 18,8· et 17,6· (2.theta., ligne CuK¿.alpha.?).

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