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H. , of 2H, m, CH 2 CO), 3.80 (6H, s, 2H, m, ArCH 2 OP), 6.24-6.44 (2H, m, CH Ar(DMP) ), 7.13-7.16 (2H, m, CH Ar(cycloSal) and CH Ar(DMP) ), 7.33 (1H, s, CH Ar(cycloSal), vol.3

, ArCH 2 OP), 32.5 (CH 2 CO), vol.34

(. Ch-ar, 3 (CH Ar(DMP) ), 104.5 (CH Ar(DMP) ), 114.9 (C Ar(DMP) ), 115.2 (C Ar(DMP) ), vol.104

C. H. Hz, C. Ar, and O. P. Ar, 4 (C Ar CH 2 OP), 123.2 (CH Ar(cycloSal) ), 127.4 (CH Ar(cycloSal) ), vol.121

(. Ch-ar, Ar OCH 3 ), 162.0 (C Ar OCH 3 ), 162.4 (C Ar OCH 3 ), C Ar OCH, vol.166, issue.5

. P-nmr, MHz, CDCl, vol.3

. F-nmr,

, OCH 2 DMP), 98.8 (CH Ar(DMP) ), 104.5 (CH Ar(DMP) ), CH Ar(cycloSal) ), vol.64, issue.3

. P-nmr, MHz, CDCl, vol.3

, HRMS (EI) + : m/z calculated for C 20 H 23 BrNO 8 PNa

, 3 -methyl)-? 2 -fluoranyl)-2-oxido-4H-benzo

, The general procedure I was applied to synthesize the compound 218f from alcohol 212 (150 mg, 0.56 mmol). The crude product was purified by automated flash chromatography (EtOAc/cyclohexane, 5 5 ! EtOAc) to give 218f as a colorless oil 149 mg

H. , CDCl 3 ): 2.78-2.91 (2H, m, CH 2 CO), 3.18 (3H, s, NCH 3 ), MHz, vol.3, issue.500

M. 2h and C. H. Ar, ArCH 2 OP), vol.6, pp.45-51

, 3 (d, 2 J C-P = 6.7 Hz, ArCH 2 OP), DMP), 98.8 (CH Ar(DMP) ), 104.7 (CH Ar(DMP) ), vol.64

, CH Ar(cycloSal) ), 123.7 (q, 1 J C-F = 271.1 Hz, C Ar CF 3 ), vol.126

C. Hz and O. P. Ar, Ar OCH 3 ), 162.4 (C Ar OCH 3 ), vol.171, p.1

, ArCH 2 OP) 6.42-6.44 (2H, m, CH Ar(DMP) ), 6.88 (5/10 of 1H, 38 (1H, m, ArCH 2 OP), 5.44-5.50 (1H, m, pp.33-38

C. H. Hz and . Ar, 2H, t, 3 J = 7.5 Hz, CH Ar(cycloSal) ), 7.10 (2H, t, 3 J = 7.5 Hz, CH Ar(cycloSal) ), 7.17 (1H, dd, 3 J = 8.9 Hz, 4 J P-H = 2.0 Hz, CH Ar(DMP) ), 7.28 (2H, m, CH Ar(cycloSal) )

, CH 2 CO), vol.55, pp.32-41

, ArCH 2 OP), 69.3 (d, 2 J C-P = 7.1 Hz, ArCH 2 OP), vol.68

. Hz, OCH 2 DMP), 98.5 (CH Ar(DMP) ), 104.1 (CH Ar(DMP) ), 117.6 (C Ar(DMP) ), vol.71

, 5 (d, 3 J C-P = 10.2 Hz, C Ar CH 2 OP), 120.8 (d, 3 J C-P = 9, vol.120

J. , 1 (d, 2 J C-P = 7.2 Hz, C Ar OP), vol.150, issue.3

. P-nmr, MHz, CDCl, vol.3, issue.9

, HRMS (EI) + : m/z calculated for C 26 H 27 NO 11 P 2 Na

N. , 4-Dimethoxybenzyl)oxy)-N-(6-methyl-2-oxido-4H-benzo

, When general procedure I was applied to synthesize compound 217b from alcohol 211 (200 mg, 0.78 mmol) a byproduct 219b was obtained. The crude product was purified by flash chromatography (EtOAc/petroleum ether, 5:5 ! EtOAc) to give 219b as a colorless oil 92 mg, 38 %) and as a mixture of two diastereoisomers

, EtOAc/ petroleum ether, vol.7

H. , ArCH 2 OP), 5.29 (1H, d, 2 J = 13.9 Hz, 3 J C-P = 8.1 Hz, ArCH 2 OP), 5.38.-5.44 (1H, m, ArCH 2 OP) 6.40-6.42 (2H, m, CH Ar(DMP) ), 6.72-6.79 (3H, m, CH Ar ), 6.88 (5/10 of 1H, d, 3 J = 6.0 Hz, CH Ar(cycloSal) ), 6.90 (5/10 of 1H, d, 3 J = 6.1 Hz, CH Ar(cycloSal) ), 7.00-7.05 (2H, m, CH Ar ), vol.7

, CDCl 3 ): 20.8 (CH 3 Ar), vol.20

, ArCH 2 OP), 69.5 (d, 2 J C-P = 7.1 Hz, ArCH 2 OP), 71.8 (OCH 2 DMP), 98.5 (CH Ar(DMP) ), 104.1 (CH Ar(DMP) ), 117.6 (C Ar(DMP) ), 118.6 (CH Ar C Ar OP), 120.0 (d, 3 J C-P = 10.0 Hz, C Ar CH 2 OP), 120.4 (d, 3 J C-P = 10.1 Hz, C Ar CH 2 OP), C Ar CH, vol.55, issue.3

J. , C Ar OP), vol.148, issue.2

C. Ar, 7 (d, 3 J C-P = 9.1 Hz, C Ar CH 2 OP), 122.1 (d, 3 J C-P = 9, CH Ar(cycloSal) ), 125.2 (CH Ar(cycloSal) ), 129.4 (C Ar Cl), 129.5 (C Ar Cl), vol.120

C. Hz and O. P. Ar, 3 (d, 2 J C-P = 7.8 Hz, C Ar OP), 148.2 (d, 2 J C-P = 6.0 Hz, C Ar OP), C Ar OCH, vol.148, issue.9

. P-nmr, MHz, CDCl, vol.3

, HRMS (EI) + : m/z calculated for C 26 H 25 Cl 2 NO 11 P 2 Na

, ]dioxaphosphinin-2-yl)oxy)-N-((2,4-dimethoxybenzyl)oxy)propanamide (219e) When general procedure I was applied to synthesize compound 217e from alcohol 211 (200 mg, 0.78 mmol) a byproduct 219e was obtained. The crude product was purified by flash chromatography (EtOAc/petroleum ether, 5:5 ! EtOAc/petroleum ether, vol.7

, Rf = 0.34 (EtOAc/ petroleum ether, vol.5

H. , (1H, m, ArCH 2 OP), 5.38-5.45 (1H, m

C. H. Hz and . Ar, 92 (5/10 of 1H, d, 3 J = 8.3 Hz, CH Ar(cycloSal) ) 7.08-7.18 (3H, m, CH Ar(cycloSal) and CH Ar(DMP), vol.6

, CDCl 3 ): 32.8 (d, 3 J C-P = 6.4 Hz, CH 2 CO), vol.55

J. , , vol.63

J. , ArCH 2 OP), 68.7 (d, 2 J C-P = 7.3 Hz, ArCH 2 OP), vol.68

;. Ch-ar, ;. Ch-ar, and . Ar, Ar(DMP) ), 117.2 (C Ar Br), 117.3 (C Ar Br), 120.6 (CH Ar C Ar OP), CH Ar C Ar OP), vol.98, issue.6

C. Hz and O. P. Ar, 4 (d, 2 J C-P = 6.7 Hz, C Ar OP), C Ar OCH, vol.149, issue.5

. P-nmr, :3) to give 219e as a colorless oil (59 mg, 15 %) and as a mixture of two diastereoisomers, EtOAc/petroleum ether, 5:5 ! EtOAc/petroleum ether, vol.3

, Rf = 0.90 (EtOAc/ petroleum ether, vol.7

H. , CH Ar(DMP) ), 6.93-6.97 (1H, m, CH Ar ), 7.13-7.16 (1H, m, CH Ar ), vol.7

, CDCl 3 ): 32.9 (d, 3 J C-P = 8.0 Hz, CH 2 CO), vol.55

J. , POCH 2 ), 68.4 (d, 2 J C-P = 6.6 Hz, ArCH 2 OP), Hz, issue.6

, DMP), 98.6 (CH Ar(DMP) ), 104.1 (CH Ar(DMP) ), 117.1 (C Ar(DMP) ), vol.119

, 127. (CH Ar ), vol.122

. P-nmr, MHz, CDCl, vol.3

. F-nmr, MHz, CDCl, vol.3

, HRMS (EI) + : m/z calculated for C 28 H 25 F 6 NO 11 P 2 Na

N. , 4-Dimethoxybenzyl)oxy)-N-(6-methoxy-2-oxido-4H-benzo

, When general procedure I was applied to synthesize compound 217g from alcohol 211 (175 mg, 0.69 mmol) a byproduct 219g was obtained. The crude product was purified by automated flash chromatography (EtOAc/petrouleum ether, 3:7 ! EtOAc) to give 219e as a colorless oil, p.12

, %) and as a mixture of two diastereoisomers

(. 2h and M. , /3 of 3H, m, NCHCH 3 *, 1/3 of 3H, m, /2 of 2H, m, CH Ar *, 1/2 of 2H, m, CH Ar ), 7.37 (5H, m, CH Ar(Bn)

, CO 2 CH 3 * and CO 2 CH 3 ), 55.8 (ArOCH 3 * and ArOCH 3 ), Ph), 78.4 (OCH 2 Ph), 114.7 (CH Ar(PMP) ), 121.3 (CH Ar(PMP) ), 128.8 (CH Ar(Bn) ), 129.0 (CH Ar(Bn) ), 129.4 (CH Ar(Bn) ), 129.5 (CH Ar(Bn) ), 129.7 (CH Ar(Bn) ), 134.3 (C Ar ), 144.5 (C Ar ), 156.5 (C Ar OCH 3 ), vol.45

. P-nmr,

, HRMS (EI) + : m/z calculated for C 21 H 27 N 2 O 8 PNa, pp.489-1376

. Methyl, Several purifications by flash chromatography and preparative TLC gave a mixture (31 mg) of the desired compound 240b and a byproduct 251* in a 50:50 ratio respectively, which was determined by NMR spectroscopy

H. , /10 of 2H, bs, CH 3 CO), 2.08 (4/10 of 2H, bs, CH 3 CO), 3.41-3.46 (2H, m, NCH 2 ), 3.68-3.76 (9/15 of 15H, m, OCH 3 *, 6/15 of 15 H, m

. Hz, /10 of 3H, bs, CH 3 CO), 3.67-3.904 (14H, m, OCH 3 and NCH 2 ), 2H, m, CH Ar(DMB) ), 6.76 (2H, m, CH Ar ), 7.05-7.10 (2H, m, CH Ar, vol.3

, CDCl 3 ): 20.4 (CH 3 CO), vol.21

. Hz, OCH 2 DMP), 71.6 (OCH 2 DMP), CH Ar(DMB) ), 104.4 (CH Ar(DMB) ), vol.45

. P-nmr,

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