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Co-Crystal Structure of Mixed Molecules

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Co-Crystal Structure of Mixed Molecules International Journal of Physical Sciences Vol. 7(10), pp. 1564 - 1570, 2 March, 2012 Available online at http://www.academicjournals.org/IJPS DOI: 10.5897/IJPS11.1772 ISSN 1992 - 1950 © 2012 Academic Journals Full Length Research Paper Co-crystal structure of mixed molecules Abdul Amir H. Kadhum2, Ahmed A. Al-Amiery1,2*, Hamdan A. Aday1, Yasamin K. Al-Majedy Ali A. Al-Temimi1, Redah I. Al-Bayati3 and Abu Bakar Mohamad2 1Department of Chemical and Process Engineering, Faculty of Engineering and Built Environment, Universiti of Kebangsaan Malaysia, Bangi, Selangor 43600, Malaysia 2Biotechnology Division, Applied Science Department, University of Technology, Baghdad 10066, Iraq. Accepted 13 January, 2012 Based on the fundamentals of organic chemistry, the approach leads to the corresponding amides in good yields which were the reaction of esters with primary amines. In our laboratory, there was no reaction when we tried to react methyl 2-(2-oxo-2H-chromen-7-yloxy)acetate with 2-(2-aminophenyl) benzothiazole). Although the spectral data was so enough for validation of the structure of the product but in the thin layer chromatography (TLC) test, there still appear two spots for the reactant (no reaction); so only X-ray single crystallography will solve this problem and identify the structure of this shiny light brown crystal. Co-crystal structure was synthesized in methanolic solution from methyl 2-(2- oxo-2H-chromen-7-yloxy)acetate and 2-(2-aminophenyl)benzothiazole). Single X-ray crystallography was studied and it was found that there was no hydrogen bonding between the molecules, moreover, the co-crystal is very stable. Key words: 2-(2-aminophenyl)benzothiazole), co-crystal, coumarins, methanol, single-crystal X-ray. INTRODUCTION During the last twenty years, the study of the biological development of coumarins as potential drugs. So far, activities of coumarin derivatives has been the aim of some coumarins, for example, warfarin, acenocoumarol, many researchers (Shih et al., 2007; Li et al., 2007; Nofal armillarisin A, hymecromone and carbochromen have et al., 2002; Al-Amiery et al., 2011; Kadhum et al., 2011a, been approved for therapeutic purposes in clinic. More 2011b). Although most of the existing natural coumarins importantly, an increasing number of coumarin have been isolated from higher plants, some of them compounds have displayed great potency in the treat- have been discovered in microorganisms, for example, ment of various types of diseases (Shi and Zhou, 2011). aminocoumarin antibiotics: novobiocin, coumermycin A1 Structure activity relationships of coumarin derivatives and chlorobiocin (produced by the actinomycete have revealed that the presence of substituted amino Streptomyces niveus) (Završniket al., 2011). Synthetic derivatives is an essential feature of their coumarin derivatives have been obtained by chemical pharmacological action. Based on these findings, we try modification of the coumarin ring. Coumarins and their to describe the synthesis of some compounds featuring derivatives have attracted considerable attention due to different heterocyclic rings fused onto the coumarin their extensively biological activities such as antibacterial, moiety with the aim of obtaining more potent pharmaco- antifungal, antiviral, anti-tubercular, anti-malarial, logically active compounds, but no reaction has been anticoagulant, anti-inflammatory, anticancer, antioxidant done. The structures of methyl 2-(3-chloro-4-methyl-2- properties and so on. Numerous efforts including the oxo-2H-chromen-7-yloxy)acetate and 2-(2-aminophenyl) separation and purification of naturally occurring benzothiazole) are shown in Figure 1. coumarins from a variety of plants as well as artificial synthesis of coumarin compounds with novel structures and properties have been focusing on the research and EXPERIMENTAL The chemicals used during synthesis were supplied by Sigma- Aldrich. Purity of the compounds was checked on thin layer chromatography (TLC) plates (Silica gel G) in the solvent system *Corresponding author. E-mail: [email protected]. benzene: ethyl acetate: methanol (40:30:30, v/v/v) and toluene: Kadhum et al. 1565 a Figure 1. The structure of the Co-crystal [Methyl2-(3-chloro-4-methyl-2-oxo-2H- chromen-7-yloxy)acetate and 2-(2- aminopheny l)benzothiazole)]. b acetone (75:25, v/v). The spots were located under ultraviolet (UV) light 254 and 365 nm. General procedure for synthesis of co-crystal Mixture of 0.05 mol of 2-(2-aminophenyl)benzothiazole and 0.05 mol of methyl 2-(3-chloro-4-methyl-2-oxo-2H-chromen-7-yloxy) acetate in methanol were refluxed for 2 h, then suitable co-crystal appeared by evaporation of methanol solution. Figure 2. FESEM for the Co-crystal [Methyl 2-(3-chloro-4- Crystal structure determination methyl-2-oxo-2H-chromen-7-yloxy)acetate and 2-(2- aminophenyl)benzothiazole)]. Diffraction data was collected on a Bruker APEX CCD area-detector diffractometer at 298(2) K on a crystal size 0.50 x 0.33 x 0.26 mm with Mo Kα radiation (Wavelength 0.71073 oA. Empirical formula C26 H21 Cl N2 O5 S, formula weight 508.96, unit cell dimensions a crystal but the results were not encouraged; all attempts = 12.611(2) A alpha = 90°, b = 7.3544(13) A beta = 99.031(4)°, c = to obtain co-crystals of theophylline, D/Ltartaric acid from 25.980(5), A gamma = 90 deg. volume 2379.7(7) A^3 Z, calculated solution failed (the outcome was theophylline). It was not density 4, 1.421 Mg/m^3. Absorption coefficient 0.290 mm^-1. F(000) 1056. Theta range for data collection 1.59 to 25.50°, limiting possible to elucidate the structure of the co-crystal using indices -15<=h<=15, -8<=k<=8, -31<=l<=23. Reflections collected / single crystal X-ray diffraction (Tomislav and William unique 13480 / 4416 [R(int) = 0.0263]. Completeness to theta = 2007; Andrei and Dimitrii, 2003; Juliana et al., 2011; Nur 25.50 99.8%. Maximum and minimum transmission 0.9285 and et al., 2010; Bohari and Nur, 2011; En-Jun et al., 2007; 0.8687. Refinement method full-matrix least-squares on F^2. Data / Sekhon 2009) Figure 2a shows an SEM image of a restraints / parameters 4416 / 0 / 321. Goodness-of-fit on F^2 1.033. Final R indices [I>2sigma(I)] R1 = 0.0520, wR2 = 0.1314. R growing co-crystal that has been synthesized from crystal indices (all data) R1 = 0.0679, wR2 = 0.1435. Largest difference grown from solution of methyl 2-(3-chloro-4-methyl-2-oxo- peak and hole 0.524 and -0.411 e.A^-3. 2H-chromen-7-yloxy)acetate and 2-(2-aminophenyl) benzothiazole), at 100 µm. Figure 2b shows the SEM image of surface morphologies of a co-crystal at 1 µm. RESULTS AND DISCUSSION From the crystal structure (Figure 3), it was found that there were two molecules in the crystal structure, first one The interest in co-crystals driven largely by new was methyl 2-(3-chloro-4-methyl-2-oxo-2H-chromen-7- opportunities in the design and construction of solid-state yloxy)acetate and the second 2-(2-aminophenyl) materials (Jones, 1997) has also brought about an benzothiazole). The crystal structure co-crystal is shown equally strong interest to discover new and efficient in Figure 3. The crystal data and experimental details are methods of co-crystal synthesis. Specifically, in addition shown in Table 1. The bond lengths and bond angles of to the traditional means of constructing co-crystals by co- co-crystal are shown in Table 2. Anisotropic displacement crystallization from solution, several research groups parameters and isotropic displacement parameters are have described the construction of two component or listed in Tables 4 and 5. The single crystal of co-crystal binary co-crystals by grinding together the two co-crystal suitable for X-ray diffraction analyses was obtained from components (Etter et al., 1993). It is too difficult to methanol solutions and the structure was examined by a synthesize co-crystal. Many researches try to build a co- single-crystal X-ray diffraction analysis. As shown in 1566 Int. J. Phys. Sci. Figure 3. The crystal structure for co-crystal [Methyl 2-(3-chloro-4- methyl-2-oxo-2H-chromen-7-yloxy)acetate and 2-(2-aminophenyl) benzothiazole)]. Table 1. Crystal data and structure refinement for Co-crystal baru441m. Crystal data Structure refinement Identification code baru441m Empirical formula C26 H21 Cl N2 O5 S Formula weight 508.96 Temperature 298(2) K Wavelength 0.71073 A a = 12.611(2) A alpha = 90° Unit cell dimensions b = 7.3544(13) A beta = 9.031(4) ° c = 25.980(5) A gamma = 90° Volume 2379.7(7) A3 Z, Calculated density 4, 1.421 Mg/m3 Absorption coefficient 0.290 mm-1 F(000) 1056 Crystal size 0.50 x 0.33 x 0.26 mm Theta range for data collection 1.59 to 25.50° Limiting indices -15<=h<=15, -8<=k<=8, -31<=l<=23 Reflections collected / unique 13480 / 4416 [R(int) = 0.0263] Completeness to theta 25.50 99.8% Max. and min. transmission 0.9285 and 0.8687 Refinement method Full-matrix least-squares on F2 Data / restraints / parameters 4416 / 0 / 321 Goodness-of-fit on F2 = 1.033 Final R indices [I>2sigma(I)] R1 = 0.0520, wR2 = 0.1314 R indices (all data) R1 = 0.0679, wR2 = 0.1435 Largest diff. peak and hole 0.524 and -0.411 e.A-3 Kadhum et al. 1567 Table 2. Atomic coordinates (x104) and equivalent isotropic Table 3. Bond lengths [A] and Bond angles displacement parameters (A2 x 103) for baru441m. U(eq) is [deg] for baru441 m. defined as one third of the trace of the orthogonalized Uij tensor. Bonds length Angle Atom X Y Z U(eq) S(1)-C(19) 1.729(3) S(1) 2810(1) 7553(1) 2187(1) 61(1) S(1)-C(20) 1.763(3) O(1) 7347(1) 3552(3) 1460(1) 57(1) O(1)-C(3) 1.360(3) O(2) 6800(2)
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