Piperidine, 1-(2-chloroethyl)-, hydrochloride → 6-{4-Hydroxy-2-[5-(2-piperidin-1-ylethoxy)-1,3-dihydroisoindol-2-yl]phenyl}-5,6,7,8-tetrahydronaphthalen-2-ol

反応式

COC1C=CC(C2CCC3C(=CC=C(OC)C=3)C2)=C(N2CC3C(=CC=C(O)C=3)C2)C=1.Cl.ClCCN1CCCCC1.C[O:42][C:43]1[CH:44]=[CH:45][C:46]([CH:67]2[CH2:76][CH2:75][C:74]3[C:69](=[CH:70][CH:71]=[C:72]([O:77]C)[CH:73]=3)[CH2:68]2)=[C:47]([N:49]2[CH2:57][C:56]3[C:51](=[CH:52][CH:53]=[C:54]([O:58][CH2:59][CH2:60][N:61]4[CH2:66][CH2:65][CH2:64][CH2:63][CH2:62]4)[CH:55]=3)[CH2:50]2)[CH:48]=1>>[OH:42][C:43]1[CH:44]=[CH:45][C:46]([CH:67]2[CH2:76][CH2:75][C:74]3[CH:73]=[C:72]([OH:77])[CH:71]=[CH:70][C:69]=3[CH2:68]2)=[C:47]([N:49]2[CH2:57][C:56]3[C:51](=[CH:52][CH:53]=[C:54]([O:58][CH2:59][CH2:60][N:61]4[CH2:66][CH2:65][CH2:64][CH2:63][CH2:62]4)[CH:55]=3)[CH2:50]2)[CH:48]=1

参加物

反応物 3

HCID 74826Piperidine, 1-(2-chloroethyl)-, hydrochloride

HCID 579338902-[5-methoxy-2-(6-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]-2,3-dihydro-1H-isoindol-5-ol

HCID 697749672-[5-methoxy-2-(6-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]-5-(2-piperidin-1-ylethoxy)-2,3-dihydro-1H-isoindole

生成物 1

HCID 579340766-{4-Hydroxy-2-[5-(2-piperidin-1-ylethoxy)-1,3-dihydroisoindol-2-yl]phenyl}-5,6,7,8-tetrahydronaphthalen-2-ol収率 59.7%

実験手順

Synthesized from 2-[5-methoxy-2-(6-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]-2,3-dihydro-1H-isoindol-5-ol and 1-(2-chloroethyl)piperidine hydrochloride according to an analogous synthetic method to Preparation Example 40, 2-[5-methoxy-2-(6-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]-5-(2-piperidin-1-ylethoxy)-2,3-dihydro-1H-isoindole (218 mg) was used according to an analogous synthetic method to Example 111 to provide the title compound (123 mg).

出典と根拠

ORDレコード: ord-5cbabd834a0b423f820b1e626570d845
出典データセット: uspto-grants-2009_11
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07612114B2

反応ノート

読み込み中…