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Tetraphos Fc(P)4
EN400-15231

Triphos Fc(P)3
EN400-15232

Triphos Fc(P)2PiPr
EN400-15233

Tetraphos Fc(P)2(P’)2
EN400-15234

Diphos Fc(P)2
EN400-15235

Diphos Fc(PFuMe)2
EN400-15236

Ligands are available in milligram and multigram quantities.
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EXAMPLES & NOTES:
(J.-C. Hierso et al. Organometallics (2003), 22(22), 4490-4499.)

  • Suzuki cross-coupling with aryl bromides at ultra-low catalyst loadings (L = Tetraphos Fc(P)4 EN400-15231)

R1
R2
Ratio S/Cat.
Yield, %

R1

C(=O)Me

R2

H

Ratio S/Cat.

100 000

Yield, %

100 (94)a

R1

CN

R2

H

Ratio S/Cat.

100 000

Yield, %

100 (87)a

R1

CF3

R2

H

Ratio S/Cat.

100 000

Yield, %

100

R1

OMe

R2

H

Ratio S/Cat.

100 000

Yield, %

77

R1

OMe

R2

H

Ratio S/Cat.

10 000

Yield, %

100 (92)a

a - isolated yield, conditions: 1 Pd / 1 Tetraphos Fc(P)4: 10-2 - 10-4 mol%; DMF or xylene, K2CO3, 130 °C, 20h.


  • Suzuki cross-coupling with aryl chlorides (L = Tetraphos Fc(P)4 EN400-15231)

R1
R2
Ratio S/Cat.
Yield, %

R1

C(=O)Me

R2

OMe

Ratio S/Cat.

1000

Yield, %

98 (88)a

R1

C(=O)Me

R2

OMe

Ratio S/Cat.

10 000

Yield, %

74

R1

CN

R2

OMe

Ratio S/Cat.

1000

Yield, %

89 (83)a

a - isolated yield, conditions: 1 Pd / 1 Tetraphos Fc(P)4 : 10-1 - 10-2 mol%; DMF or xylene, K2CO3, 130 °C, 20h.


  • Heck reaction at ultralow catalyst loadings (L = Tetraphos Fc(P)4 EN400-15231)

Aryl Halide
Alkene
Ratio S/Cat.
Yield, %
Time, h

Aryl Halide

PhI

Alkene

n-BuOCOCH=CH2

Ratio S/Cat.

1000 000

Yield, %

100 (85)a

Time, h

48

Aryl Halide

4-MeOC6H4Br

Alkene

n-BuOCOCH=CH2

Ratio S/Cat.

10 000

Yield, %

100 (88)a

Time, h

48

Aryl Halide

4-MeOC6H4Br

Alkene

C6H5CH=CH2

Ratio S/Cat.

100 000

Yield, %

65a

Time, h

20

Aryl Halide

4-CH(O)C6H4Br

Alkene

n-BuOCH=CH2

Ratio S/Cat.

250

Yield, %

100 (83)a

Time, h

20

Aryl Halide

4-CH(O)C6H4Br

Alkene

n-BuOCH=CH2

Ratio S/Cat.

1000

Yield, %

41a

Time, h

20

a - isolated yield, conditions: 1 Pd / 1 Tetraphos Fc(P)4, Xylene, K2CO3, 130 °C.


  • Alkynylation of aryl halides (Heck-Sonogashira reaction) under low (10-1 to 10-4 mol%) catalyst loadings in the presence of a Triphos Fc(P)2PiPr EN400-15233 with TONs up to 250000. Copper-free coupling using phenyl- acetylene is also accessible in good yield.

    J.-C. Hierso, V. Ivanov et al., Organic Letters (2004), 6(20), 3473-3476.
    H. Doucet, J.-C. Hierso, Angewandte Chemie International Edition (2007), 46, 834-871.

Aryl Halide
Alkene
Ratio S/Cat.
Yield, %

Aryl Halide

PhI

Alkene

phenylacetylene

Ratio S/Cat.

100 000

Yield, %

95

Aryl Halide

4-Bromoacetophenone

Alkene

phenylacetylene

Ratio S/Cat.

100 000

Yield, %

94

Aryl Halide

4-Bromobenzonitrile

Alkene

phenylacetylene

Ratio S/Cat.

10 000

Yield, %

89

Aryl Halide

4-Chlorobenzonitrile

Alkene

phenylacetylene

Ratio S/Cat.

250

Yield, %

86a

Aryl Halide

4-Bromoanisole

Alkene

phenylacetylene

Ratio S/Cat.

250

Yield, %

93

Aryl Halide

4-Bromoacetophenone

Alkene

but-1-yn-4-ol

Ratio S/Cat.

250

Yield, %

92b

aReaction performed without CuI. bReaction performed at 100 °C / Conditions: catalyst {Pd(C3H5)Cl}2/Triphos Fc(P)2Pi-Pr 1/2, aryl halide (1 mmol), alkyne (2 mmol), CuI (0.05 mmol), K2CO3 (2 mmol), DMF, 130 °C, 20 h, isolated yields.
  • Selective Amination of allylic acetates under low catalyst loadings in the presence of ferrocenyldiphosphine Diphos Fc(PFuMe)2 EN400-15236

    J.-C. Hierso et al. Advanced Synthesis and Catalysis (2005), 347(9), 1198-1202.
    J.-C. Hierso, H. Doucet et al. Tetrahedron (2005), 61, 9759-9766.

Acetate
Amine
Ratio S/Cat.
Conditions
Conversion, %
Selectivity
TOF (h-1)

Acetate

Allyl acetate

Amine

aniline

Ratio S/Cat.

100

Conditions

Rt, 1h

Conversion, %

100

Selectivity

96/4

TOF (h-1)

10 000

Acetate

Allyl acetate

Amine

piperidine

Ratio S/Cat.

10 000

Conditions

Rt, 1h

Conversion, %

100

Selectivity

-

TOF (h-1)

5 000

Acetate

Allyl acetate

Amine

morpholine

Ratio S/Cat.

10 000

Conditions

Rt, 2h

Conversion, %

85

Selectivity

100

TOF (h-1)

4 250

Acetate

Allyl acetate

Amine

diisopropylamine

Ratio S/Cat.

1 000

Conditions

80 °C 2h

Conversion, %

96

Selectivity

100

TOF (h-1)

480

Acetate

Hex-2-en-1-yl acetate

Amine

pyrrolidine

Ratio S/Cat.

1 000

Conditions

50 °C, 20h

Conversion, %

100

Selectivity

93/7(lin/br)

TOF (h-1)

-

Acetate

Hex-2-en-1-yl acetate

Amine

morpholine

Ratio S/Cat.

1 000

Conditions

50 °C, 20h

Conversion, %

98

Selectivity

94/6(lin/br)

TOF (h-1)

-

Acetate

Cinnamyl acetate

Amine

pyrrolidine

Ratio S/Cat.

1 000

Conditions

50 °C, 20h

Conversion, %

100

Selectivity

94/6(lin/br)

TOF (h-1)

2 600

Acetate

Cinnamyl acetate

Amine

morpholine

Ratio S/Cat.

1 000

Conditions

50 °C, 20h

Conversion, %

100

Selectivity

93/7(lin/br)

TOF (h-1)

4 800

Acetate

Cinnamyl acetate

Amine

diethylamine

Ratio S/Cat.

1 000

Conditions

Rt, 20h

Conversion, %

100

Selectivity

94/6(lin/br)

TOF (h-1)

7 600

Acetate

Geranyl acetate

Amine

morpholine

Ratio S/Cat.

1 000

Conditions

80 °C, 3h

Conversion, %

100

Selectivity

98

TOF (h-1)

33

Catalyst {Pd(C3H5)Cl}2 / Diphos Fc(PFuMe)2 Conditions: S/C = 250-10000, T = 25°C-50 °C, 2 equiv. amine, 1 to 20 h.

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