Table 6.

C–N-bond-formation cross coupling of N-protected 4-bromo-7-azaindoles 1 with amino acid (esters) 6.

Entry	7-Azaindole 1	Amino acid (ester) 6	Product 7a	Time (h)	Yield (%)b	ee (%)d
1	1c	6a	7a	2	traces	–
2	1c	6b	7b	2	70	98.79
3	1c	6c	7c	2	72	–
4	1c	6d	7d	3	65	95.48
5	1d	6b	7e	2	71	98.91
6	1d	6c	7f	2.1	72	–
7	1d	6e	7g	2	70	–
8	1c	6f	–	5	0	–
9	1c	6g	–	5	0	–
10	1c	6h	–	5	0	–

^aAll reactions were carried out at 100 °C. N-substituted 4-bromo-azaindoles 1c or 1d (1.0 mmol), amino acid (esters) (1.2 mmol), Cs₂CO₃ (3.0 mmol), Pd₂(dba)₃ (5 mol %) and Xantphos (10 mol %) were used for all the reactions. ^bYields reported are isolated yields. ^cDesulfonation reaction takes place. ^dee was determined by chiral HPLC.