Table 2.
4 °C Reactions | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|
Entry | i | i+1 | i+2 | i+3 | i+4 | i+5 | 1 (%) | 3 (%) | 5 (%) | ee (%) |
1 | Pmh | Asn(Trt) | Aib | Ser(t-Bu) | DTyr(t-Bu) | Phe | 0.2 | 24.8 | 75.0 | 56 |
2 | Pmh | Asn(Trt) | Aib | Ser(t-Bu) | DPhe | Phe | 0.2 | 24.1 | 75.7 | 52 |
3 | Pmh | His(Trt) | Aib | Ser(t-Bu) | DPhe | Phe | 0.2 | 21.9 | 77.9 | 51 |
4 | Pmh | Asn(Trt) | Leu | Ser(t-Bu) | DTyr(t-Bu) | Phe | 0.1 | 26.4 | 73.5 | 51 |
5 | Pmh | Asn(Trt) | Leu | Thr(t-Bu) | DTyr(t-Bu) | Phe | 0.2 | 23.3 | 76.5 | 51 |
6* | Pmh | Asn(Trt) | Leu | Ser(t-Bu) | DPhe | Phe | 0.1 | 11.7 | 88.2 | 51 |
*Entry 9, Table 1 | ||||||||||
−20 °C Reactions | ||||||||||
7 | Pmh | Asn(Trt) | Aib | Ser(t-Bu) | DTyr(t-Bu) | Phe | 3.2 | 71.9 | 24.9 | 79 |
8 | Pmh | His(Trt) | Aib | Ser(t-Bu) | DPhe | Phe | 2.4 | 73.5 | 24.1 | 78 |
9 | Pmh | Asn(Trt) | Aib | Thr(t-Bu) | DPhe | Phe | 0.2 | 53.5 | 46.3 | 78 |
10 | Pmh | Asn(Trt) | Aib | Ser(t-Bu) | DPhe | Phe | 3.5 | 74.8 | 21.7 | 77 |
11* | Pmh | Asn(Trt) | Leu | Ser(t-Bu) | DPhe | Phe | 0.6 | 62.8 | 36.6 | 70 |
12 | Pmh | Asn(Trt) | Leu | Ser(t-Bu) | DTyr(t-Bu) | Phe | 12.6 | 73.2 | 14.2 | 68 |
*Entry 9, Table 1 |