公开(公告)号：US3655716A

公开(公告)日：1972-04-11

申请号：US3655716D

申请日：1970-06-01

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  WEIGELE MANFRED

IPC: C07C255/24 ,  C07D239/42 ,  C07C121/42

CPC classification number: C07C255/00

Abstract: THIS INVENTION IS DIRECTED TO A PROCESS FOR THE PREPARATION OF AMINOMETHYLENE AMALONONITRILE FROM DIALKYL AMINOACRYLONITRILE INCLUDING INTERMEDIATES THEREIN. AMINOMETHYLENE MALONONITRILE IS A KNOWN COMPOUND WHICH IS A VALUABLE INTERMEDIATE IN THE SYNTHESIS OF THIAMINE.

公开(公告)号：US3562280A

公开(公告)日：1971-02-09

申请号：US3562280D

申请日：1967-08-30

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  SCHENKER FAUSTO EUGENIO

IPC: A61K31/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10 ,  C07D35/10

CPC classification number: A61K31/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10 ,  Y02P20/55

Abstract: NOVEL PHARMACOLOGICALLY ACTIVE 8-(LOWER ALKOXY)-1,23,4-TETRAHYDROISOQUINOLINES, 8-(LOWER ALKOXY)-1 AND/OR 2(LOWER ALKYL)-1,2,3,4-TETRAHYDROISOQUINOLINES AND INTERMEDIATES THEREFOR, ARE PREPARED UTILIZING, FOR EXAMPLE, 8ISOQUINOLINOL AS A STARTING MATERIAL. THE PHARMACOLOGICALLY ACTIVE COMPOUNDS OF THE INVENTION ARE USEFUL AS HYPOTENSIVE AGENTS.

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：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：US3917646A

公开(公告)日：1975-11-04

申请号：US44771174

申请日：1974-03-04

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  WEIGELE MANFRED

IPC: C07C45/74 ,  C07C49/683 ,  C07C49/697 ,  C07C49/753 ,  C07C49/755 ,  C07C65/40 ,  C07C229/38 ,  C07D303/32 ,  C07D311/76 ,  C07D317/60 ,  C07D493/10 ,  G01N31/22 ,  G01N33/48 ,  G01N33/52 ,  G01N33/68 ,  C07D209/18 ,  C07D307/88 ,  C07D317/50

CPC classification number: C07D493/10 ,  C07C45/74 ,  C07C49/683 ,  C07C49/697 ,  C07C49/753 ,  C07C49/755 ,  C07C65/40 ,  C07C229/38 ,  C07D303/32 ,  C07D311/76 ,  C07D317/60 ,  G01N31/22 ,  G01N33/48 ,  G01N33/52 ,  G01N33/6809

Abstract: A novel class of reagents react with primary amine-containing compounds, preferably polypeptides and amino acids, to form highly fluorescent products. This reaction serves as a basis for a rapid and highly sensitive assay method for primary aminecontaining compounds.

Abstract translation: 一类新的试剂与含伯胺的化合物，优选多肽和氨基酸反应，形成高度荧光的产物。 该反应作为用于含伯胺化合物的快速和高灵敏度测定方法的基础。

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：US3901888A

公开(公告)日：1975-08-26

申请号：US41373573

申请日：1973-11-07

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  WEIGELE MANFRED

IPC: C07D239/42

CPC classification number: C07C255/00

Abstract: This invention is directed to a process for the preparation of 4-amino-2-methylpyrimidine 5-carboxamide from 2-cyano-3-di-(lower alkyl)amino acrolein. The 4-amino-2-methylpyrimidine 5carboxamide is a known compound which is a valuable intermediate in the synthesis of thiamine.

公开(公告)号：US3900511A

公开(公告)日：1975-08-19

申请号：US48066074

申请日：1974-06-19

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  WEIGELE MANFRED

IPC: C07C120/00 ,  C07C121/20

CPC classification number: C07C255/00

Abstract: This invention is directed to a process for the preparation of aminomethylene malononitrile from dialkyl aminoacylonitrile including intermediates therein. Aminomethylene malononitrile is a known compound which is a valuable intermediate in the synthesis of thiamine.

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.