Crystalline and amorphous forms of dezocine analog hydrochloride

文档序号:1431709 发布日期:2020-03-17 浏览:22次 中文

阅读说明:本技术 地佐辛类似物盐酸盐的晶型及无定型 (Crystalline and amorphous forms of dezocine analog hydrochloride ) 是由 张杨 伍文韬 李志祥 于 2018-06-29 设计创作,主要内容包括:本发明涉及地佐辛类似物盐酸盐的晶型及无定型,具体涉及式(I)所示化合物的晶型及式(Ⅱ)所示化合物的无定型,其晶型的X-射线粉末衍射图谱包含在2θ值为13.1°±0.2°,16.8±0.2°和18.5±0.2°的特征峰,其无定型的X-射线粉末衍射图谱如图1所示。(The invention relates to a crystal form and an amorphous form of dezocine analogue hydrochloride, in particular to a crystal form of a compound shown in a formula (I) and an amorphous form of a compound shown in a formula (II), wherein an X-ray powder diffraction pattern of the crystal form comprises characteristic peaks with 2 theta values of 13.1 +/-0.2 degrees, 16.8 +/-0.2 degrees and 18.5 +/-0.2 degrees, and the amorphous X-ray powder diffraction pattern is shown in figure 1.)

A crystal form of a compound shown in a formula (I),

Figure PCTCN2018093721-APPB-100001

its X-ray powder diffraction pattern contains characteristic peaks at 2 theta values of 13.07 DEG + -0.2 DEG, 16.84 DEG + -0.2 DEG and 18.51 DEG + -0.2 deg.

A crystalline form according to claim 1 having an X-ray powder diffraction pattern comprising characteristic peaks, in terms of 2 Θ, at 13.07 ° ± 0.2 °, 15.30 ° ± 0.2 °, 16.84 ° ± 0.2 °, 18.51 ° ± 0.2 °, 21.44 ° ± 0.2 °, 23.18 ° ± 0.2 °, 24.04 ° ± 0.2 ° and 26.20 ° ± 0.2 °.

The crystalline form of claim 2 having an X-ray powder diffraction pattern as shown in figure 4.

The crystalline form of claim 1, wherein the DSC curve of the crystalline form comprises two endothermic peaks at 73.71 ℃ ± 3 ℃ and 245.82 ℃ ± 3 ℃.

The crystalline form of claim 4, wherein the crystalline form has a DSC curve as shown in figure 5.

The crystalline form of claim 1, wherein the crystalline form has a TGA profile with a weight loss of 5.812% at 120.00 ℃ ± 3 ℃; at 200.12 ℃. + -. 3 ℃ the weight loss was 6.5748%.

The crystalline form of claim 6, wherein the TGA curve of the crystalline form is set forth in figure 6.

Amorphous form of the compound of formula (II),

Figure PCTCN2018093721-APPB-100002

the X-ray powder diffraction pattern is shown in figure 1.

The amorphous form of claim 8, wherein the amorphous form of the MDSC curve has a glass transition at 79.07 ℃ ± 3 ℃.

The amorphous form of claim 9, wherein the amorphous MDSC profile is shown in figure 2.

The amorphous form of claim 8, wherein the TGA profile of the amorphous form has a weight reduction of 4.270% at 120.00 ℃ and a weight reduction of 5.1553% at 199.60 ℃ ± 3 ℃.

The amorphous form according to claim 11, wherein the TGA profile of the amorphous form is shown in figure 3.

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