公开(公告)号：US3553223A

公开(公告)日：1971-01-05

申请号：US3553223D

申请日：1968-01-05

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  MOHACSI ERNEST

IPC: C07D211/70 ,  C07D211/82 ,  C07D213/30 ,  C07D221/26 ,  C07D39/00

CPC classification number: C07D213/30 ,  C07D211/70 ,  C07D211/82 ,  C07D221/26

Abstract: THERE IS DESCRIBED A PROCESS FOR THE ACID CATALYZED CYCLIZATION OF 2- (4-METHOXYBENZYL)-3,4-DIALKYL-1,2,5,6TETRAHYDROPYRIDINES SUBSTITUTED AT THE NITROGEN ATOM WITH ELECTRON WITHDRAWING GROUPS, TO THE CORRESPONDING BENZOMORPHAN COMPOUNDS UTILIZING NOVEL INTERMEDIATES. THE BENZOMORPHAN COMPOUNDS SO PRODUCED ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF PHARMACEUTICALLY ACTIVE COMPOUNDS, E.G., KNOWN BENZOMORPHAN DERIVATIVES EXHIBITING ANALGESIC ACTIVITY.

公开(公告)号：US3914234A

公开(公告)日：1975-10-21

申请号：US44608974

申请日：1974-02-26

Applicant: HOFFMANN LA ROCHE

Inventor： MOHACSI ERNEST ,  LEIMGRUBER WILLY

IPC: C07D221/26 ,  C07D221/28 ,  A61K31/485

CPC classification number: C07D221/26 ,  C07D221/28

Abstract: Novel 2-lower alhoxy morphinan derivatives which may bear a variety of N-substituents, are disclosed. These morphinans are useful as analgesic agents and are also useful as antagonists of certain strong analgesics such as morphine.

Abstract translation: 公开了可能具有多种N-取代基的新的2-低级甲氧基吗啡喃衍生物。 这些吗啡可用作止痛剂，也可用作某些强镇痛药如吗啡的拮抗剂。

公开(公告)号：US3912761A

公开(公告)日：1975-10-14

申请号：US50812874

申请日：1974-09-23

Applicant: HOFFMANN LA ROCHE

Inventor： DEN HOLLANDER CHARLES WILLIAM ,  LEIMGRUBER WILLY ,  MOHACSI ERNEST

IPC: C07H7/027 ,  C07D317/26

CPC classification number: C07H7/027

Abstract: Racemic modifications of optically active amines are treated with (-)-di-O-isopropylidene-2-keto-L-gulonic acid to form diastereomeric salts. The so-formed diastereomeric salts are separated and chemically decomposed to give the desired enantiomers of the amine. The resolving agent, (-)-di-0isopropylidene-2-keto-L-gulonic acid, is recovered by precipitation from aqueous solution.

Abstract translation: 用（ - ） - 二-O-异亚丙基-2-酮-L-古洛糖酸处理光学活性胺的外消旋体，形成非对映异构体盐。 将如此形成的非对映异构体盐分离并化学分解，得到所需胺的对映异构体。 通过从水溶液中沉淀来回收拆分剂（ - ） - 二-O-异亚丙基-2-酮-L-古洛糖酸。

公开(公告)号：US3914232A

公开(公告)日：1975-10-21

申请号：US44608374

申请日：1974-02-26

Applicant: HOFFMANN LA ROCHE

Inventor： MOHACSI ERNEST ,  LEIMGRUBER WILLY

IPC: C07D221/26 ,  C07D221/28 ,  A61K31/485

CPC classification number: C07D221/26 ,  C07D221/28

Abstract: Novel 2- and 4-acyloxy morphinan derivatives, which may bear a variety of N-substituents, are disclosed. These morphinans are useful as analgesic agents and are also useful as antagonists of certain strong analgesics such as morphine.

Abstract translation: 公开了可能具有各种N-取代基的新的2-和4-酰氧基吗啡喃衍生物。 这些吗啡可用作止痛剂，也可用作某些强镇痛药如吗啡的拮抗剂。

公开(公告)号：US3904632A

公开(公告)日：1975-09-09

申请号：US50813074

申请日：1974-09-23

Applicant: HOFFMANN LA ROCHE

Inventor： HOLLANDER CHARLES WILLIAM DEN ,  LEIMGRUBER WILLY ,  MOHACSI ERNEST

IPC: C07H7/027 ,  C07D221/28 ,  C07D407/04

CPC classification number: C07H7/027

Abstract: Racemic modifications of optically active amines are treated with (-)-di-O-isopropylidene-2-keto-L-gulonic acid to form diastereomeric salts. The so-formed diastereomeric salts are separated and chemically decomposed to give the desired enantiomers of the amine. The resolving agent, (-)-di-Oisopropylidene-2-keto-L-gulonic acid, is recovered by precipitation from aqueous solution.

公开(公告)号：US3875209A

公开(公告)日：1975-04-01

申请号：US35686873

申请日：1973-05-03

Applicant: HOFFMANN LA ROCHE

Inventor： MOHACSI ERNEST ,  LEIMGRUBER WILLY

IPC: C07C69/003 ,  C07D207/24 ,  C07D211/76 ,  C07C69/78

CPC classification number: C07D207/24 ,  C07D211/76

Abstract: Process for preparing an ester by reacting a carboxylic acid with an O-lower alkyl imino ether.

Abstract translation: 通过使羧酸与O-低级烷基亚氨基醚反应来制备酯的方法。

公开(公告)号：US3920746A

公开(公告)日：1975-11-18

申请号：US43364374

申请日：1974-01-16

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  MOHACSI ERNEST

IPC: C07C41/01 ,  C07C91/02 ,  C07C93/02 ,  C07C93/10 ,  C07C95/02

CPC classification number: C07C41/01 ,  C07D489/02 ,  C07C43/205 ,  C07C43/202

Abstract: Tertiary-butyl aryl ethers are prepared by reacting the corresponding phenol or phenolic compound with N,Ndimethylformamide di-t-butyl acetal under basic conditions. The preparation of substantially pure N,N-dimethylformamide di-tbutyl acetal by the acid-catalyzed trans-acetalization of N,Ndimethylformamide dimethyl acetal with t-butanol is also described.

公开(公告)号：US3914233A

公开(公告)日：1975-10-21

申请号：US44608474

申请日：1974-02-26

Applicant: HOFFMANN LA ROCHE

Inventor： MOHACSI ERNEST ,  LEIMGRUBER WILLY

IPC: C07D221/26 ,  C07D221/28 ,  A61K31/485

CPC classification number: C07D221/26 ,  C07D221/28

Abstract: Novel 4-hydroxy morphinan derivatives, which may bear a variety of N-substituents, are disclosed. These morphinans are useful as analgesic agents and are also useful as antagonists of certain strong analgesics such as morphine.

Abstract translation: 公开了可以具有多种N-取代基的新型4-羟基吗啡喃衍生物。 这些吗啡可用作止痛剂，也可用作某些强镇痛药如吗啡的拮抗剂。

公开(公告)号：US3682925A

公开(公告)日：1972-08-08

申请号：US3682925D

申请日：1969-01-30

Applicant: HOFFMANN LA ROCHE

Inventor： HOLLANDER CHARLES WILLIAM DEN ,  LEIMGRUBER WILLY ,  MOHACSI ERNEST

IPC: C07D217/24 ,  C07B57/00 ,  C07C67/00 ,  C07C209/00 ,  C07C211/27 ,  C07C213/00 ,  C07C213/10 ,  C07C215/08 ,  C07C215/36 ,  C07C227/34 ,  C07C229/02 ,  C07D217/20 ,  C07D221/28 ,  C07D35/28 ,  C07D43/28

CPC classification number: C07D217/20 ,  C07C215/08 ,  C07D221/28

Abstract: Racemic modifications of optically active amines are treated with (-)-di-O-isopropylidene-2-keto-L-gulonic -keto-L-gulonic acid to form diastereomeric salts. The so-formed diastereomeric salts are separated and chemically decomposed to give the desired enantiomers of the amine. The resolving agent, (-)-di-Oisopropylidene-2-keto-L-gulonic acid, is recovered by precipitation from aqueous solution.

Abstract translation: 用（ - ） - 二-O-异亚丙基-2-酮-L-古洛酮 - 酮-L-古洛糖酸处理光学活性胺的外消旋体改性以形成非对映体盐。 将如此形成的非对映异构体盐分离并化学分解，得到胺的所需对映异构体。 拆分剂（ - ） - 二-O-异亚丙基-2-酮-L-古洛糖酸通过从水溶液中沉淀回收。

公开(公告)号：US3634429A

公开(公告)日：1972-01-11

申请号：US3634429D

申请日：1969-09-30

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  MOHACSI ERNEST

IPC: C07D221/28 ,  C07D43/28

CPC classification number: C07D221/28

Abstract: THERE IS DESCRIBED A PROCESS FOR THE ACID CATALYZED CYCLIZATION OF 1-(P-METHOXYBENZYL) - 1,2,3,4,5,6,7,8 - OCTAHYDROISOQUINOLINES SUBSTITUTED IN THE 2-POSITION WITH ELECTRON WITHDRAWING GROUPS TO THE CORRESPONDING MORPHINAN COMPOUNDS, BY UTILIZING AS THE CATALYST SULFURIC ACID, PHOSPHORIC ACID, POLYPHOSPHORIC ACID OR MIXTURES THEREOF. THE MORPHINAN COMPOUNDS SO PRODUCED ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF 3-METHOXY-N-METHYL MORPHINANS, KNOWN COMPOUNDS WITH ANALGESIC AND ANTITUSSIVE PROPERTIES.