Literature DB >> 21754471

3-{(E)-[1-(2-Hy-droxy-phen-yl)ethyl-idene]amino}-1-(2-methyl-phen-yl)thio-urea.

Md Abdus Salam, Md Abu Affan, Mohd Razip Asaruddin, Seik Weng Ng, Edward R T Tiekink.   

Abstract

In the title thio-urea derivative, C(16)H(17)N(3)OS, the hy-droxy- and methyl-substituted benzene rings form dihedral angles of 9.62 (12) and 55.69 (6)°, respectively, with the central CN(3)S chromophore (r.m.s. deviation = 0.0117 Å). An intra-molecular O-H⋯N hydrogen bond ensures the coplanarity of the central atoms. The H atoms of the NH groups are syn and the conformation about the N=C double bond [1.295 (4) Å] is E. In the crystal, helical supra-molecular chains sustained primarily by N-H⋯S hydrogen bonds are found. Additional stabilization is provided by C-H⋯π and π-π [ring centroid(hy-droxy-benzene)⋯ring centroid(methyl-benzene) = 3.8524 (18) Å] inter-actions.

Entities:  

Year:  2011        PMID: 21754471      PMCID: PMC3089068          DOI: 10.1107/S1600536811013729

Source DB:  PubMed          Journal:  Acta Crystallogr Sect E Struct Rep Online        ISSN: 1600-5368


Related literature

For pharmaceutical applications of thio­ruea derivatives, see: Venkatachalam et al. (2004 ▶); Bruce et al. (2007 ▶). For related thio­urea structures, see: Normaya et al. (2011 ▶); Salam et al. (2011 ▶); Dzulkifli et al. (2011 ▶).

Experimental

Crystal data

C16H17N3OS M = 299.39 Monoclinic, a = 14.6966 (8) Å b = 7.3586 (4) Å c = 14.0926 (8) Å β = 94.358 (5)° V = 1519.66 (15) Å3 Z = 4 Mo Kα radiation μ = 0.22 mm−1 T = 100 K 0.30 × 0.10 × 0.05 mm

Data collection

Agilent Supernova Dual diffractometer with an Atlas detector Absorption correction: multi-scan (CrysAlis PRO; Agilent, 2010 ▶) T min = 0.419, T max = 1.000 7614 measured reflections 3375 independent reflections 2094 reflections with I > 2σ(I) R int = 0.066

Refinement

R[F 2 > 2σ(F 2)] = 0.060 wR(F 2) = 0.174 S = 1.00 3375 reflections 201 parameters 3 restraints H atoms treated by a mixture of independent and constrained refinement Δρmax = 0.34 e Å−3 Δρmin = −0.34 e Å−3 Data collection: CrysAlis PRO (Agilent, 2010 ▶); cell refinement: CrysAlis PRO; data reduction: CrysAlis PRO; program(s) used to solve structure: SHELXS97 (Sheldrick, 2008 ▶); program(s) used to refine structure: SHELXL97 (Sheldrick, 2008 ▶); molecular graphics: ORTEP-3 (Farrugia, 1997 ▶) and DIAMOND (Brandenburg, 2006 ▶); software used to prepare material for publication: publCIF (Westrip, 2010 ▶). Crystal structure: contains datablocks global, I. DOI: 10.1107/S1600536811013729/hg5025sup1.cif Structure factors: contains datablocks I. DOI: 10.1107/S1600536811013729/hg5025Isup2.hkl Additional supplementary materials: crystallographic information; 3D view; checkCIF report
C16H17N3OSF(000) = 632
Mr = 299.39Dx = 1.309 Mg m3
Monoclinic, P21/cMo Kα radiation, λ = 0.71073 Å
Hall symbol: -P 2ybcCell parameters from 1905 reflections
a = 14.6966 (8) Åθ = 2.8–29.3°
b = 7.3586 (4) ŵ = 0.22 mm1
c = 14.0926 (8) ÅT = 100 K
β = 94.358 (5)°Prism, light-yellow
V = 1519.66 (15) Å30.30 × 0.10 × 0.05 mm
Z = 4
Agilent Supernova Dual diffractometer with an Atlas detector3375 independent reflections
Radiation source: SuperNova (Mo) X-ray Source2094 reflections with I > 2σ(I)
MirrorRint = 0.066
Detector resolution: 10.4041 pixels mm-1θmax = 27.5°, θmin = 2.8°
ω scansh = −14→19
Absorption correction: multi-scan (CrysAlis PRO; Agilent, 2010)k = −9→7
Tmin = 0.419, Tmax = 1.000l = −18→15
7614 measured reflections
Refinement on F2Primary atom site location: structure-invariant direct methods
Least-squares matrix: fullSecondary atom site location: difference Fourier map
R[F2 > 2σ(F2)] = 0.060Hydrogen site location: inferred from neighbouring sites
wR(F2) = 0.174H atoms treated by a mixture of independent and constrained refinement
S = 1.00w = 1/[σ2(Fo2) + (0.0769P)2] where P = (Fo2 + 2Fc2)/3
3375 reflections(Δ/σ)max < 0.001
201 parametersΔρmax = 0.34 e Å3
3 restraintsΔρmin = −0.34 e Å3
Geometry. All s.u.'s (except the s.u. in the dihedral angle between two l.s. planes) are estimated using the full covariance matrix. The cell s.u.'s are taken into account individually in the estimation of s.u.'s in distances, angles and torsion angles; correlations between s.u.'s in cell parameters are only used when they are defined by crystal symmetry. An approximate (isotropic) treatment of cell s.u.'s is used for estimating s.u.'s involving l.s. planes.
Refinement. Refinement of F2 against ALL reflections. The weighted R-factor wR and goodness of fit S are based on F2, conventional R-factors R are based on F, with F set to zero for negative F2. The threshold expression of F2 > 2σ(F2) is used only for calculating R-factors(gt) etc. and is not relevant to the choice of reflections for refinement. R-factors based on F2 are statistically about twice as large as those based on F, and R- factors based on ALL data will be even larger.
xyzUiso*/Ueq
S10.46230 (5)0.24817 (10)0.38597 (5)0.0188 (2)
O10.21619 (14)0.2307 (3)0.31997 (15)0.0250 (5)
H1O0.2693 (11)0.261 (4)0.308 (2)0.038*
N10.33770 (15)0.3710 (3)0.22261 (17)0.0182 (6)
N20.42781 (16)0.4196 (3)0.21980 (18)0.0190 (6)
H2N0.4433 (19)0.497 (3)0.1764 (16)0.023*
N30.57409 (16)0.4362 (3)0.27942 (17)0.0197 (6)
H3N0.5801 (19)0.496 (4)0.2259 (13)0.024*
C10.1592 (2)0.2588 (4)0.2410 (2)0.0229 (7)
C20.0685 (2)0.2066 (5)0.2458 (3)0.0309 (8)
H20.04960.15440.30270.037*
C30.0062 (2)0.2298 (5)0.1692 (3)0.0331 (9)
H3A−0.05530.19270.17320.040*
C40.0327 (2)0.3073 (5)0.0857 (3)0.0320 (8)
H4−0.01040.32360.03270.038*
C50.1220 (2)0.3603 (4)0.0806 (2)0.0260 (8)
H5A0.13960.41420.02360.031*
C60.18777 (19)0.3372 (4)0.1568 (2)0.0200 (7)
C70.28345 (19)0.3879 (4)0.1464 (2)0.0189 (7)
C80.3131 (2)0.4548 (4)0.0530 (2)0.0229 (7)
H8A0.37950.44320.05250.034*
H8B0.29570.58270.04450.034*
H8C0.28340.38240.00120.034*
C90.48965 (19)0.3751 (4)0.2920 (2)0.0174 (7)
C100.65424 (19)0.4166 (4)0.3422 (2)0.0172 (7)
C110.6563 (2)0.4776 (4)0.4351 (2)0.0201 (7)
H110.60240.52420.45920.024*
C120.7355 (2)0.4712 (4)0.4928 (2)0.0252 (7)
H12A0.73640.51120.55700.030*
C130.8147 (2)0.4057 (4)0.4568 (2)0.0253 (7)
H130.87030.40350.49600.030*
C140.8128 (2)0.3441 (4)0.3647 (2)0.0231 (7)
H140.86710.29740.34140.028*
C150.73287 (19)0.3485 (4)0.3047 (2)0.0195 (7)
C160.7318 (2)0.2841 (4)0.2034 (2)0.0260 (8)
H16A0.78150.19690.19740.039*
H16B0.74010.38820.16150.039*
H16C0.67330.22530.18510.039*
U11U22U33U12U13U23
S10.0225 (4)0.0163 (4)0.0179 (4)−0.0009 (3)0.0039 (3)−0.0001 (3)
O10.0214 (11)0.0291 (13)0.0247 (13)−0.0029 (10)0.0027 (10)−0.0005 (10)
N10.0150 (12)0.0148 (13)0.0247 (15)−0.0010 (10)0.0019 (10)−0.0010 (11)
N20.0179 (13)0.0166 (14)0.0222 (15)−0.0023 (10)0.0002 (11)0.0044 (11)
N30.0187 (13)0.0205 (14)0.0199 (15)−0.0006 (11)0.0016 (11)0.0052 (11)
C10.0245 (16)0.0172 (16)0.0269 (18)0.0046 (13)0.0018 (13)−0.0085 (14)
C20.0234 (17)0.030 (2)0.040 (2)−0.0028 (14)0.0098 (15)−0.0020 (16)
C30.0198 (17)0.031 (2)0.049 (2)−0.0018 (14)0.0039 (16)−0.0077 (17)
C40.0248 (18)0.0298 (19)0.040 (2)0.0018 (15)−0.0039 (15)0.0006 (17)
C50.0242 (17)0.0207 (17)0.032 (2)0.0010 (14)−0.0026 (14)−0.0014 (15)
C60.0174 (15)0.0158 (16)0.0266 (18)−0.0010 (12)0.0003 (13)−0.0037 (13)
C70.0209 (15)0.0104 (15)0.0250 (18)0.0038 (12)0.0004 (13)−0.0030 (13)
C80.0248 (16)0.0192 (17)0.0247 (18)−0.0002 (13)0.0021 (13)−0.0036 (14)
C90.0180 (15)0.0151 (15)0.0197 (16)0.0034 (12)0.0045 (12)−0.0028 (13)
C100.0185 (15)0.0126 (15)0.0205 (17)−0.0006 (12)0.0014 (12)0.0014 (12)
C110.0272 (16)0.0095 (14)0.0239 (18)0.0015 (13)0.0045 (13)−0.0009 (13)
C120.0354 (19)0.0158 (16)0.0235 (18)−0.0033 (14)−0.0037 (14)0.0013 (14)
C130.0249 (17)0.0192 (17)0.030 (2)−0.0021 (13)−0.0091 (14)0.0055 (14)
C140.0171 (15)0.0183 (16)0.034 (2)0.0001 (13)0.0034 (13)0.0026 (15)
C150.0262 (16)0.0132 (15)0.0200 (17)−0.0058 (13)0.0063 (13)−0.0003 (13)
C160.0275 (17)0.0240 (18)0.0276 (19)−0.0018 (14)0.0094 (14)−0.0020 (14)
S1—C91.694 (3)C6—C71.473 (4)
O1—C11.357 (4)C7—C81.500 (4)
O1—H1O0.842 (10)C8—H8A0.9800
N1—C71.295 (4)C8—H8B0.9800
N1—N21.375 (3)C8—H8C0.9800
N2—C91.352 (4)C10—C111.383 (4)
N2—H2N0.880 (10)C10—C151.400 (4)
N3—C91.344 (3)C11—C121.369 (4)
N3—C101.426 (4)C11—H110.9500
N3—H3N0.882 (10)C12—C131.391 (4)
C1—C21.394 (4)C12—H12A0.9500
C1—C61.411 (4)C13—C141.373 (4)
C2—C31.372 (5)C13—H130.9500
C2—H20.9500C14—C151.395 (4)
C3—C41.390 (5)C14—H140.9500
C3—H3A0.9500C15—C161.503 (4)
C4—C51.376 (4)C16—H16A0.9800
C4—H40.9500C16—H16B0.9800
C5—C61.400 (4)C16—H16C0.9800
C5—H5A0.9500
C1—O1—H1O108 (2)H8A—C8—H8B109.5
C7—N1—N2119.0 (2)C7—C8—H8C109.5
C9—N2—N1120.6 (2)H8A—C8—H8C109.5
C9—N2—H2N119 (2)H8B—C8—H8C109.5
N1—N2—H2N119.3 (19)N3—C9—N2113.2 (2)
C9—N3—C10127.7 (2)N3—C9—S1124.3 (2)
C9—N3—H3N115.6 (19)N2—C9—S1122.4 (2)
C10—N3—H3N116.7 (19)C11—C10—C15121.0 (3)
O1—C1—C2116.8 (3)C11—C10—N3120.9 (3)
O1—C1—C6123.2 (3)C15—C10—N3117.9 (3)
C2—C1—C6120.0 (3)C12—C11—C10120.5 (3)
C3—C2—C1120.8 (3)C12—C11—H11119.7
C3—C2—H2119.6C10—C11—H11119.7
C1—C2—H2119.6C11—C12—C13119.5 (3)
C2—C3—C4120.2 (3)C11—C12—H12A120.2
C2—C3—H3A119.9C13—C12—H12A120.2
C4—C3—H3A119.9C14—C13—C12120.1 (3)
C5—C4—C3119.4 (3)C14—C13—H13120.0
C5—C4—H4120.3C12—C13—H13120.0
C3—C4—H4120.3C13—C14—C15121.5 (3)
C4—C5—C6122.1 (3)C13—C14—H14119.3
C4—C5—H5A119.0C15—C14—H14119.3
C6—C5—H5A119.0C14—C15—C10117.4 (3)
C5—C6—C1117.6 (3)C14—C15—C16121.1 (3)
C5—C6—C7120.1 (3)C10—C15—C16121.5 (3)
C1—C6—C7122.3 (3)C15—C16—H16A109.5
N1—C7—C6115.1 (3)C15—C16—H16B109.5
N1—C7—C8123.9 (3)H16A—C16—H16B109.5
C6—C7—C8120.9 (3)C15—C16—H16C109.5
C7—C8—H8A109.5H16A—C16—H16C109.5
C7—C8—H8B109.5H16B—C16—H16C109.5
C7—N1—N2—C9−168.5 (3)C10—N3—C9—N2178.6 (3)
O1—C1—C2—C3−179.9 (3)C10—N3—C9—S1−3.6 (4)
C6—C1—C2—C30.3 (5)N1—N2—C9—N3−178.5 (2)
C1—C2—C3—C4−0.5 (5)N1—N2—C9—S13.7 (4)
C2—C3—C4—C50.1 (5)C9—N3—C10—C11−56.4 (4)
C3—C4—C5—C60.6 (5)C9—N3—C10—C15129.0 (3)
C4—C5—C6—C1−0.8 (5)C15—C10—C11—C12−0.5 (4)
C4—C5—C6—C7177.0 (3)N3—C10—C11—C12−174.9 (3)
O1—C1—C6—C5−179.4 (3)C10—C11—C12—C131.1 (4)
C2—C1—C6—C50.3 (4)C11—C12—C13—C14−1.5 (5)
O1—C1—C6—C72.8 (5)C12—C13—C14—C151.2 (5)
C2—C1—C6—C7−177.4 (3)C13—C14—C15—C10−0.6 (4)
N2—N1—C7—C6−178.4 (2)C13—C14—C15—C16178.8 (3)
N2—N1—C7—C81.2 (4)C11—C10—C15—C140.2 (4)
C5—C6—C7—N1176.2 (3)N3—C10—C15—C14174.8 (3)
C1—C6—C7—N1−6.1 (4)C11—C10—C15—C16−179.2 (3)
C5—C6—C7—C8−3.4 (4)N3—C10—C15—C16−4.6 (4)
C1—C6—C7—C8174.3 (3)
D—H···AD—HH···AD···AD—H···A
O1—H1o···N10.842 (10)1.81 (2)2.551 (3)145 (3)
N2—H2n···S1i0.880 (10)2.508 (16)3.323 (2)154 (3)
N3—H3n···S1i0.882 (10)2.485 (17)3.286 (3)151 (2)
C8—H8b···Cg1i0.982.593.501 (3)155
Table 1

Hydrogen-bond geometry (Å, °)

Cg1 is the centroid of the C10–C15 ring.

D—H⋯AD—HH⋯ADAD—H⋯A
O1—H1o⋯N10.84 (1)1.81 (2)2.551 (3)145 (3)
N2—H2n⋯S1i0.88 (1)2.51 (2)3.323 (2)154 (3)
N3—H3n⋯S1i0.88 (1)2.49 (2)3.286 (3)151 (2)
C8—H8b⋯Cg1i0.982.593.501 (3)155

Symmetry code: (i) .

  5 in total

1.  Effect of stereochemistry on the anti-HIV activity of chiral thiourea compounds.

Authors:  T K Venkatachalam; C Mao; Fatih M Uckun
Journal:  Bioorg Med Chem       Date:  2004-08-01       Impact factor: 3.641

2.  A short history of SHELX.

Authors:  George M Sheldrick
Journal:  Acta Crystallogr A       Date:  2007-12-21       Impact factor: 2.290

3.  3-(2-Hy-droxy-phen-yl)-1-{(E)-[1-(pyrazin-2-yl)ethyl-idene]amino}-thio-urea monohydrate.

Authors:  Erna Normaya; Yang Farina; Siti Nadiah Abd Halim; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-23

4.  1-Cyclo-hexyl-3-{(E)-[1-(pyridin-2-yl)ethyl-idene]amino}-thio-urea.

Authors:  Md Abdus Salam; Md Abu Affan; Fasihuddin B Ahmad; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-23

5.  3-[(E)-(4-Chloro-benzyl-idene)amino]-1-phenyl-thio-urea.

Authors:  Nur Nadia Dzulkifli; Yang Farina; Bohari M Yamin; Ibrahim Baba; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-12
  5 in total

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