참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Potassium Carbonate | HCID 11430 | — |
| 반응물 | 2-Thiopheneboronic acid | HCID 2733960 | — |
| 반응물 | (S)-Methyl 2-((tert-butoxycarbonyl)amino)-3-(4-(((trifluoromethyl)sulfonyl)oxy)phenyl)propanoate | HCID 10455198 | — |
| 촉매 | HCID 178418397 | HCID 178418397 | — |
| 용매 | Toluene | HCID 1140 | — |
| 용매 | Dimethylformamide toluene | HCID 21735183 | — |
| 생성물 | N-(tert-butoxycarbonyl)-4-(2-thienyl)-L-phenylalanine methyl ester | HCID 10309111 | 62.6% |
반응 단계
To a mixture of 2-thienylboronic acid (1.135 g) and anhydrous K2CO3 (2.23 g) in toluene/DMF (75 mL/7.5 mL) under N2 was added a solution of N-(tert-butoxycarbonyl)-O-(trifluoromethanesulfonyl)-L-tyrosine methyl ester (3.42 g) in 5 mL of toluene. Pd(PPh3)4 (1.4 g) was added and the mixture was heated at 80° C. for 24 h. After usual work-up as shown in Example 1 the crude material was purified by flash column chromatography (silica gel; eluent: EtOAc/hexane 1:3) to yield N-(tert-butoxycarbonyl)-4-(2-thienyl)-L-phenylalanine methyl ester (1.81 g). ESMS: m/z 362 (MH+).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US06855843B2 |
|---|
| 출처 데이터셋 | uspto-grants-2005_02 |
|---|
| ORD ID | ord-1db0bfad9af543919c7b8344aca7a271 |
|---|
| 출처 메모 | uspto-grants-2005_02 |
|---|
