Synlett 2010(1): 67-72  
DOI: 10.1055/s-0029-1218564
LETTER
© Georg Thieme Verlag Stuttgart ˙ New York

Borylated Thiaporphyrin Building Blocks for the Synthesis of Unsymmetrical Phenyl-Bridged Porphyrin Dyads

M. Yedukondalu, M. Ravikanth*
Department of Chemistry, Indian Institute of Technology, Bombay, Powai, Mumbai 400 076, India
e-Mail: ravikanth@chem.iitb.ac.in;
Further Information

Publication History

Received 1 September 2009
Publication Date:
10 December 2009 (online)

Abstract

meso-(4-Borylphenyl)thiaporphyrin building blocks with N3S and N2S2 porphyrin cores have been synthesized using two different approaches and used for the synthesis of meso-meso- and β-meso-1,4-phenylene-bridged unsymmetrical porphyrin dyads containing two different porphyrin subunits.

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Experimental Procedure and Spectroscopic Data for Selected Compounds. Diol 3: Thiophene mono-alcohol 4 (0.96 g, 4.7 mmol), TMEDA (1.76 mL, 11.7 mmol) and n-BuLi (7.34 mL, ˜15% in hexane) were added successively to freshly distilled anhydrous Et2O (30 mL) in a 250-mL three-necked, round-bottomed flask and stirred for 45 min under nitrogen atmosphere at 0 ˚C. An ice-cold solution of 4-formylboronic ester (1.25 g, 5.7 mmol) in THF (30 mL) was added and the mixture was stirred for an additional 45 min. The reaction was quenched with ice-cold NH4Cl (50 mL, ˜1 M) and the organic layer was separated from the aqueous layer. The aqueous layer was extracted several times with Et2O and the combined organic layers were washed thoroughly with water and brine and dried with anhydrous Na2SO4. The solvent was removed on a rotary evaporator under reduced pressure to afford the crude compound. TLC analysis showed three minor and one major spot corresponding to the unreacted 4-formylphenylboronic ester, unreacted mono-alcohol 4, unidentified compound and the desired diol 3. The crude compound was subjected to silica gel column chromatography (petroleum ether-EtOAc, 80:20). The aldehyde, the mono-alcohol 4 and the minor unidentified compound were removed and the desired diol 3 was collected (petroleum ether-EtOAc, 70:30) as yellow oily liquid (0.60 g, 30%). ¹H NMR (400 MHz, CDCl3): δ = 1.03 (s, 6 H, CH3), 2.34 (s, 3 H, CH3), 3.50 (br s, 2 H, OH), 3.76 (s, 4 H, CH2), 5.92-5.96 (m, 2 H, CHOH), 6.67-6.69 (m, 2 H, thiophene), 7.28-7.30 (m, 2 H, ArH), 7.40 (d, J = 7.0 Hz, 2 H, ArH), 7.77-7.79 (m, 4 H, ArH). ¹³C NMR (100 MHz, CDCl3): δ = 22.5, 65.8, 71.5, 120.1, 124.3, 124.5, 125.5, 128.1, 129.3, 134.6, 136.1, 139.5, 140.2, 143.7, 145.6, 146.0, 149.7, 152.8, 155.6 ppm. ES-MS: m/z calcd for C24H27BO4S: 422.1; found: 351.1 (100) [M - C5H11]+. Anal. Calcd for C24H27BO4S: C, 68.25; H, 6.44. Found: C, 68.30; H, 6.37.
Porphyrin 6: A solution of diol 3 (0.5 g, 1.2 mmol), p-tolualdehyde (0.3 mL, 2.4 mmol) and pyrrole (0.25 mL, 3.6 mmol) in CH2Cl2 (300 mL) were condensed in the presence of BF3˙OEt2 (396 mL, 2.5 M) under an inert atmosphere. After 1 h, DDQ (0.272 g, 1.2 mmol) was added and the reaction was stirred in open air for an additional 1 h. TLC analysis indicated the formation of a mixture of four porphyrins: tetra(p-tolyl)porphyrin (H2TTP), the desired mono-functionalized 21-thiaporphyrin boronic acid 6 and a cis and trans mixture of 21,23-dithiaporphyrin boronic acid. The crude mixture of porphyrins was subjected to silica gel column chromatography and the fast moving H2TTP was removed with petroleum ether-CH2Cl2 (80:20). The desired 6 was collected as a second band using petroleum ether-CH2Cl2 (40:60) and the cis and trans mixture of porphyrins was collected in CH2Cl2. The solvent was removed on a rotary evaporator to afford H2TTP (3%), the desired compound 6 (8%) and the cis and trans mixture (<1%). ¹H NMR (400 MHz, CDCl3): δ = -2.69 (s, 1 H, NH), 2.69 (s, 9 H, CH3), 7.23 (d, J = 8.2 Hz, 2 H, ArH), 7.54 (d, J = 7.6 Hz, 4 H, ArH), 7.61 (d, J = 7.6 Hz, 2 H, ArH), 8.06-8.14 (m, 8 H, ArH), 8.67 (d, J = 4.6 Hz, 2 H, β-pyrrole), 8.68 (d, J = 4.6 Hz, 2 H, β-pyrrole), 8.93 (s, 2 H, β-pyrrole), 9.75 (s, 2 H, β-thiophene). ¹³C NMR (100 MHz, CDCl3): δ = 21.8, 31.2, 103.2, 120.9, 121.3, 123.6, 128.4, 128.5, 129.2, 130.4, 133.2, 134.3, 134.7, 135.2, 135.9, 136.9, 138.1, 138.4, 145.8, 148.3, 154.1, 156.8, 157.1, 157.6. ES-MS: m/z calcd for C47H36BN3O2S: 717.3; found: 718.3 (100%) [M + 1]+. UV/Vis (CH2Cl2): λmax (log ε) = 431 (5.89), 515 (4.59), 551 (4.16), 619 (3.66), 680 nm (3.95).
Porphyrin 7: Samples of diol 3 (0.4 g, 0.95 mmol) and tripyrrane 5 (0.398 g, 0.95 mmol) in CH2Cl2 (250 mL) were condensed in the presence of BF3˙OEt2 (200 mL, 2.5 M) under inert atmosphere for 1 h. DDQ (0.216 g, 0.95 mmol) was added and stirring was continued for additional 1 h in open air. TLC analysis showed the formation of the desired product 7 as the sole product. Chromatography on silica (petroleum ether-CH2Cl2, 50:50) gave porphyrin 7 as a purple solid (0.08 g, 11%). ¹H NMR (400 MHz, CDCl3): δ = 2.70 (s, 9 H, CH3), 7.21 (d, J = 7.6 Hz, 2 H, ArH), 7.61 (d, J = 7.6 Hz, 6 H, ArH), 8.08 (d, J = 7.6 Hz, 6 H, ArH), 8.23 (s, 2 H, ArH), 8.67 (s, 4 H, β-pyrrole), 9.95 (s, 4 H, β-thiophene). ¹³C NMR (100 MHz, CDCl3): δ = 22.6, 22.8, 31.1, 31.5, 128.0, 129.5, 133.6, 134.7, 134.9, 135.1, 135.7, 136.1, 138.0, 146.8, 147.6, 148.5, 148.7, 149.8, 150.9, 155.1, 157.1. ES-MS: m/z calcd for C47H35BN2O2S2: 734.2; found: 735.6 (100%) [M + 1]+. UV/Vis (CH2Cl2): λmax (log ε) = 437 (5.83), 515 (4.67), 550 (4.27), 634 (3.55), 698 nm (4.01).
Porphyrin 1: Method 1: Compound 6 (0.04 g, 0.055 mmol) was treated with 2,2-dimethylpropane-1,3-diol (0.009 g, 0.083 mmol) in THF (15 mL) at r.t. for 2 h. Flash column chromatography (CH2Cl2) afforded porphyrin boronic ester 1 in 97% yield.
Borylated thiaporphyrin building blocks for the synthesis of unsymmetrical phenyl bridged porphyrin dyads: Method 2: The meso-brominated thiaporphyrin 10 (0.03 g, 0.044 mmol) was treated with phenyl diboronic ester 12 (0.04 g, 0.13 mmol) in toluene-triethylamine (5:1) in the presence of catalytic amounts of Pd(PPh3)4 (0.005 g, 0.004 mmol) and Cs2CO3 (0.016 g, 0.066 mmol) at 80 ˚C for 2 h. After standard work-up, the crude compound was purified by silica gel column chromatography (petroleum ether-CH2Cl2, 60:40) to afford the porphyrin boronic ester 1 in 51% yield. ¹H NMR (400 MHz, CDCl3): δ = -2.69 (s, 1 H, NH), 1.16 (s, 6 H, CH3), 2.69 (s, 9 H, CH3), 3.93 (s, 4 H, CH2), 7.23 (d, J = 8.2 Hz, 2 H, ArH), 7.54 (d, J = 7.6 Hz, 4 H, ArH), 7.61 (d, J = 7.6 Hz, 2 H, ArH), 8.06-8.14 (m, 8 H, ArH), 8.67 (d, J = 4.6 Hz, 2 H, β-pyrrole), 8.68 (d, J = 4.6 Hz, 2 H, β-pyrrole), 8.93 (s, 2 H, β-pyrrole), 9.75 (s, 2 H, β-thiophene). ¹³C NMR (100 MHz, CDCl3): δ = 21.8, 31.2, 103.2, 120.9, 121.3, 123.6, 128.4, 128.5, 129.2, 130.4, 133.2, 134.3, 134.7, 135.2, 135.9, 136.9, 138.1, 138.4, 145.8, 148.3, 154.1, 156.8, 157.1, 157.6. ES-MS: m/z calcd for C52H44BN3O2S: 785.3; found: 786.4 (100%) [M + 1]+. Anal. Calcd for C52H44BN3O2S: C, 79.48; H, 5.64; N, 5.35. Found: C, 79.53; H, 5.68; N, 5.30.
Porphyrin 2: Porphyrin 2 was synthesized in 58% yield following same experimental conditions used for the synthesis of porphyrin 1. ¹H NMR (400 MHz, CDCl3): δ = 1.16 (s, 6 H, CH3), 2.70 (s, 9 H, CH3), 3.96 (s, 4 H, CH2), 7.21 (d, J = 7.6 Hz, 2 H, ArH), 7.61 (d, J = 7.6 Hz, 6 H, ArH), 8.08 (d, J = 7.6 Hz, 6 H, ArH), 8.23 (s, 2 H, ArH), 8.67 (s, 4 H, β-pyrrole), 9.95 (s, 4 H, β-thiophene). ¹³C NMR (100 MHz, CDCl3): δ = 22.6, 22.8, 31.1, 31.5, 128.0, 129.5, 133.6, 134.7, 134.9, 135.1, 135.7, 136.1, 138.0, 146.8, 147.6, 148.5, 148.7, 149.8, 150.9, 155.1, 157.1. MALDI-TOF: m/z calcd for C52H43BN2O2S2: 802.3; found: 802.1 (100%) [M]+. Anal. Calcd for C52H43BN2O2S2: C, 77.79; H, 5.40; N, 3.49. Found: C, 77.85; H, 5.38; N, 3.52.
General procedure for dyads 13 and 14: Samples of meso-bromo N3S porphyrin 10/β-bromo ZnN4 porphyrin 15 and N2S2 porphyrin boronic ester 2 or N2S2 porphyrin boronic acid 7 were dissolved in anhydrous toluene-triethylamine (6 mL, 5:1) in a 25-mL two-necked, round-bottomed flask under a nitrogen atmosphere. Cs2CO3 (1.5 equiv) followed by Pd(PPh3)4 (0.1 equiv) were added and the resulting mixture was heated at 80 ˚C for 4 h. After work-up, the crude compound was subjected to silica gel chromatography to afford dyads 13 and 14 as purple solids in reasonable yields.
Spectral data for compounds 13 and 14:
Compound 13: Yield: 78%. ¹H NMR (400 MHz, CDCl3):
δ = -2.55 (s, 1 H, NH), 2.64 (t, J = 7.9 Hz, 18 H, CH3), 7.47 (d, J = 7.6 Hz, 2 H, ArH), 7.50-7.54 (m, 10 H, ArH), 7.58 (d, J = 7.6 Hz, 2 H, ArH), 7.99 (d, J = 7.9 Hz, 2 H, ArH), 8.03-8.12 (m, 12 H, ArH), 8.52 (d, J = 4.6 Hz, 1 H, β-pyrrole), 8.59 (s, 2 H, β-pyrrole), 8.61-8.62 (m, 2 H, β-pyrrole), 8.64 (d, J = 4.6 Hz, 1 H, β-pyrrole), 8.70 (d, J = 4.3 Hz, 1 H,
β-pyrrole), 8.87 (dd, J = 10.7, 2.1 Hz, 2 H, β-pyrrole), 9.19 (d, J = 4.6 Hz, 1 H, β-pyrrole), 9.59 (s, 2 H, β-thiophene), 9.63 (d, J =4.9 Hz, 1 H, β-thiophene), 9.69 (d, J =5.2 Hz, 1 H, β-thiophene), 9.79 (d, J =5.2 Hz, 1 H, β-thiophene), 10.22 (d, J =5.2 Hz, 1 H, β-thiophene). ¹³C NMR (100 MHz, CDCl3): δ = 21.7, 22.9, 34.0, 53.6, 114.3, 115.1, 121.3, 127.5, 128.6, 129.3, 131.9, 132.0, 134.4, 134.8, 135.8, 137.2, 140.1, 146.5, 148.9, 150.5, 150.9, 154.9. MALDI-TOF: m/z calcd for C88H63N5S3: 1285.4; found: 1285.6 (100%) [M]+. Anal. Calcd for C88H63N5S3: C, 82.15; H, 4.94; N, 5.44. Found: C, 82.21; H, 4.85; N, 5.41.
Compound 14: Yield: 58%. ¹H NMR (400 MHz, CDCl3):
δ = 2.63 (s, 21 H, CH3), 7.35-7.39 (m, 4 H, ArH), 7.52-7.54 (m, 8 H, ArH), 7.62 (d, J = 7.7 Hz, 6 H, ArH), 7.69-7.71 (m, 6 H, ArH), 7.93 (d, J =7.0 Hz, 2 H, ArH), 8.05 (d, J =7.0 Hz, 2 H, ArH), 8.13 (d, J = 7.4 Hz, 4 H, ArH), 8.32 (d, J = 4.0 Hz, 2 H, β-pyrrole), 8.69-8.71 (m, 4 H, β-pyrrole), 8.74-8.76 (m, 2 H, β-pyrrole), 8.84 (s, 1 H, β-pyrrole), 9.42 (s, 1 H, β-pyrrole), 9.54 (s, 1 H, β-pyrrole), 9.70 (s, 2 H, β-thiophene), 9.73 (d, J = 5.2 Hz, 2 H, β-thiophene). ¹³C NMR (100 MHz, CDCl3): δ = 23.7, 110.8, 114.8, 118.2, 126.3, 128.5, 128.3, 129.0, 129.4, 130.6, 131.0, 132.0, 132.7, 133.6, 134.4, 135.2, 135.7, 136.3, 137.0, 137.6, 141.3, 143.1, 146.3, 155.5. MALDI-TOF: m/z calcd for C96H70N6S2Zn: 1434.4; found: 1434.5 (100%) [M]+. Anal. Calcd for C96H70N6S2Zn: C, 80.23; H, 4.91; N, 5.85. Found: C, 80.15; H, 5.01; N, 5.78.